Search Result
Results for "
Antagonistic peptide
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P2276A
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- HY-P0099
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nAChR
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Others
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Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .
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- HY-P5971A
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Melanocortin Receptor
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Metabolic Disease
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TCMCB07 TFA, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia .
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- HY-P4874
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Melanocortin Receptor
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Metabolic Disease
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ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity .
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- HY-P5971
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Mifomelatide
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Melanocortin Receptor
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Metabolic Disease
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TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia. TCMCB07 has potential transport capabilities .
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- HY-103304
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Others
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Neurological Disease
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CGRP antagonist 4 is an antagonist of calcitonin gene-related peptide (CGRP) receptor. CGRP antagonist 4 shows the highest affinity for CGRP receptors in the human brain. CGRP antagonist 4 can be used to study the binding properties of non-peptide calcitonin gene-related peptide (CGRP) receptor antagonist (gepants) in rat, pig and human menes .
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- HY-P2268
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Amyloid-β
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Inflammation/Immunology
Cancer
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RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities .
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- HY-P2268A
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Amyloid-β
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Inflammation/Immunology
Cancer
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RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities .
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- HY-176505
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Opioid Receptor
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Neurological Disease
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NOP antagonist 1 (Compound (-)-31) is a nociceptin opioid peptide (NOP) antagonist with a Kb of 8.65 nM. NOP antagonist 1 can be used for neuropsychiatric disorders research .
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- HY-P11035
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Ephrin Receptor
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Neurological Disease
Cancer
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APY-d3 is a EphA4-LBD antagonistic peptide with a Kd of 138 nM. APY-d3 is constrained into a bioactive β-hairpin conformation via a head-to-tail disulfide bond. APY-d3 can be used for cancers like gastric and pancreatic cancers and neurodegenerative diseases like amyotrophic lateral sclerosis and Alzheimer’s disease research .
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- HY-P5359
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- HY-P1376
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mAChR
Adrenergic Receptor
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Endocrinology
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G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
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- HY-P5889
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Thrombin
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Cardiovascular Disease
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Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent .
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- HY-P11214
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H-TL1
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TNF Receptor
Integrin
NF-κB
ERK
p38 MAPK
JNK
Interleukin Related
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Inflammation/Immunology
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Hydrostatin-TL1 (H-TL1), a nine-amino-acid peptide, is a TNF-α antagonist. Hydrostatin-TL1 can be isolated from the venom gland of sea snake Hydrophis cyanocinctus. H-TL1 competitively inhibits the interaction between TNF-α/TNFR1 and attenuates the cytotoxicity and inflammation of TNF-α. Hydrostatin-TL1 can be used for TNF-α-associated inflammatory diseases, such as rheumatoid arthritis, osteoporosis and inflammatory bowel disease (IBD) research .
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- HY-P4111
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CXCR
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Cancer
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Peptide R, a cyclic peptide, is a specific CXCR4 antagonist. Peptide R shows outstanding capacities to profoundly remodel the tumor stroma. Peptide R has the potential for tumor research .
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- HY-P10957
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MBX 1416
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GLP Receptor
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Metabolic Disease
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Imapextide is a glucagon-like peptide-1 (GLP-1) receptor antagonist that can be used in hypoglycemia research .
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- HY-P10973
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CXCR
ERK
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Cancer
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Peptide R analogue 10 (compound 10) is an analog of the CXCR4 antagonist peptide Peptide R (HY-P4111) with stronger antagonistic potency, specificity and plasma stability. Peptide R analogue 10 can inhibit CXCL12-mediated cell migration, ERK phosphorylation and CXCR4 internalization. Peptide R analogue 10 can be used in the study of CXCR4 overexpressing leukemia and colon cancer .
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- HY-103473A
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Boc-Met-Leu-Phe-OH TFA
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Formyl Peptide Receptor (FPR)
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Inflammation/Immunology
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Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations .
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- HY-P1376A
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mAChR
Adrenergic Receptor
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Endocrinology
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G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
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- HY-139035
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CRFR
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Neurological Disease
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CRHR1 antagonist 1 (compound 10a) is a non-peptide corticotropin-releasing hormone type 1 receptor (CRHR1) antagonist. CRHR1 antagonist 1 can be utilized in mental disorders research .
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- HY-P2612A
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TNF Receptor
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Others
Cancer
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WP9QY, TNF-a Antagonist, TNF-a Antagonist is a biological active peptide. (This cyclic peptide is designed to mimic the most critical tumor necrosis factor (TNF) recognition loop on TNF receptor I. It prevents interactions of TNF with its receptor. This TNF antagonist is a useful template for the development of small molecular inhibitors to prevent both inflammatory bone destruction and systemic bone loss in rheumatoid arthritis.)
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- HY-P2612
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TNF Receptor
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Others
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WP9QY, TNF-a Antagonist, TNF-a Antagonist is a biological active peptide. (This cyclic peptide is designed to mimic the most critical tumor necrosis factor (TNF) recognition loop on TNF receptor I. It prevents interactions of TNF with its receptor. This TNF antagonist is a useful template for the development of small molecular inhibitors to prevent both inflammatory bone destruction and systemic bone loss in rheumatoid arthritis.)
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- HY-174986
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CGRP Receptor
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Cardiovascular Disease
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CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a Ki of 0.029 nM. CGRP antagonist 7 Inhibit the production of cyclic adenosine monophosphate (cAMP) with an IC50 of 1.5 nM. CGRP antagonist 7 can be used for the study of migraine .
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- HY-16027
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GnRH Receptor
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Endocrinology
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Acyline, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels .
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- HY-P2669
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- HY-145353
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- HY-P4111A
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CXCR
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Cancer
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Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. Peptide R (TFA) shows outstanding capacities to remodel the tumor stroma. Peptide R (TFA) can be used for solid tumor (glioblastoma, etc.) research .
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- HY-10308
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Others
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Metabolic Disease
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Lefradafiban is an orally active glycoprotein IIb/IIIa receptor antagonist. Lefradafiban can be metabolized to its active form, Fradafiban, a non-peptide GP IIb/IIIa receptor antagonist .
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- HY-P10938
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- HY-16027A
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GnRH Receptor
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Endocrinology
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Acyline TFA, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels .
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- HY-P5188A
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- HY-P5171
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Wnt
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Cancer
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MDGCEL is a WNT5A peptide, that acts as a WNT5A mimicks and exhibits WNT5A antagonistic activity .
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- HY-P1988
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- HY-105506
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Angiotensin Receptor
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Cardiovascular Disease
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EXP-7711 is a non peptide angiotensin II (Ang II) AT1 receptor antagonist. EXP-7711’s affinity for wild-type AT1 receptor (Ki =180 nM) is lower than peptide antagonists, but higher than losartan (Ki = 12 nM). EXP-7711 can be used for research on cardiovascular conditions .
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- HY-P10204
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Wnt
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Cancer
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FZD7 antagonist 1 (peptide 34) is a dFz7-21 analogue. FZD7 antagonist 1 is an FZD7 antagonist that inhibits the wnt3a with IC50 value of 9.2 nM. FZD7 antagonist 1 blocks TcdB−FZD interaction via targeting FZD receptors .
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- HY-115975
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Bombesin Receptor
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Cancer
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GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity .
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- HY-P11011
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Pep R54; CXCR4 antagonist peptide 19
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CXCR
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Cancer
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Peptide R54 (Pep R54; CXCR4 antagonist peptide 19) is an antagonistic peptide targeting CXCR4 with significant anticancer activity. Peptide R54 inhibits CXCR4-dependent cell migration, epithelial-mesenchymal transition, and lung metastasis development, with better serum stability and higher CXCR4 affinity than the lead compound (IC50=20 nM). Peptide R54 synergizes with anti-PD-1 therapy to exert anti-tumor activity in vivo, enhances granzyme activity, and reduces infiltration of Foxp3 cells. Peptide R54 can be used in the study of colon cancer, ovarian cancer, and melanoma .
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- HY-P1014
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- HY-P1572
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Renin
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Inflammation/Immunology
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Handle region peptide, rat is a prorenin receptor antagonist, suppresses the progression of diabetic nephropathy and has anti-inflammatory in the eye.
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- HY-P4157
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MDM-2/p53
Apoptosis
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Metabolic Disease
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FOXO4-DRI is a cell-permeable peptide antagonist that blocks the interaction of FOXO4 and p53. FOXO4-DRI is a senolytic peptide that induces apoptosis of senescent cells .
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- HY-P4157A
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MDM-2/p53
Apoptosis
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Metabolic Disease
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FOXO4-DRI acetate is a cell-permeable peptide antagonist that blocks the interaction of FOXO4 and p53. FOXO4-DRI acetate is a senolytic peptide that induces apoptosis of senescent cells .
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- HY-135108
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Neurokinin Receptor
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Neurological Disease
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QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC50 of 4.7 μM .
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- HY-10095A
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BIBN-4096 hydrochloride; BIBN4096BS hydrochloride
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CGRP Receptor
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Neurological Disease
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Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP .
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- HY-P2319
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p38 MAPK
JNK
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Inflammation/Immunology
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OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
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- HY-10095
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BIBN-4096; BIBN 4096BS
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CGRP Receptor
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Neurological Disease
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Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP .
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- HY-P2319A
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p38 MAPK
JNK
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Inflammation/Immunology
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OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
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- HY-15016
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Oxytocin Receptor
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Endocrinology
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(E/Z)-OT-R antagonist 1 is a mixture of E/Z forms of OT-R antagonist 1 (HY-15015). OT-R antagonist 1 is a novel, potent, selective non-peptide OT-R antagonist that inhibits oxytocin-induced intracellular Ca 2+ activation (IC50 = 8 nM) .
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- HY-156293
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Formyl Peptide Receptor (FPR)
Apoptosis
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Cancer
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FPR1 antagonist 1 (compound 24a) is a formyl peptide receptor 1 (FPR1) antagonist with an IC50 of 25 nM. FPR1 antagonist 1 inhibits cell growth through a combined effect on cell proliferation and apoptosis and reduces cell migration, while inducing an increase in angiogenesis .
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- HY-156294
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Formyl Peptide Receptor (FPR)
Apoptosis
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Cancer
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FPR1 antagonist 2 (compound 25b) is a formyl peptide receptor 1 (FPR1) antagonist with an IC50 of 70 nM. FPR1 antagonist 2 inhibits cell growth through a combined effect on cell proliferation and apoptosis and reduces cell migration, while inducing an increase in angiogenesis .
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- HY-103473
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- HY-P3557
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- HY-100356
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CNS 1102 free base
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iGluR
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Neurological Disease
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Aptiganel (CNS 1102 (free base)), peptide, is a noncompetitive NMDA antagonist with cerebroprotective effects. Aptiganel can be used for the research of stroke .
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- HY-P3227
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XJ735
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Integrin
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Inflammation/Immunology
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Cyclo(Ala-Arg-Gly-Asp-Mamb) is a selective RGD peptide antagonist and has the potential for Pulmonary arterial hypertension
Research .
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- HY-135773
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Prostaglandin Receptor
PDK-1
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Cardiovascular Disease
Inflammation/Immunology
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CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist . CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation .
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- HY-N2600
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Bombesin Receptor
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Cancer
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Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells .
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- HY-101116
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GCGR
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Metabolic Disease
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GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM .
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- HY-N14982
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- HY-105137
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- HY-P1023
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GCGR
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Metabolic Disease
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VIP(6-28)(human, rat, porcine, bovine) is an effective antagonist of the actions of exogenous vasoactive intestinal peptide (VIP) on cAMP.
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- HY-101844
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Bombesin Receptor
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Cancer
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ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
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- HY-P10577
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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RAG8 peptide is an antagonist for protease-activated receptor 4 (PAR 4), which inhibits late-stage platelet activation, and reduces thrombosis without altering hemostasis or increasing bleeding risk. RAG8 peptide can be used for atherosclerosis research .
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- HY-P10949
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Glycoprotein VI
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Cardiovascular Disease
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Pep-10L peptide is a glycoprotein VI (GPVI) antagonist with Ki values of 180, 225, and 179 μM for CPR, GPO-1, and Type 1 collagen, respectively. Pep-10L peptide has anti-thrombotic effects .
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- HY-P1271
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Catestatin (cattle)
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nAChR
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Cardiovascular Disease
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Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
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- HY-108555
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM. .
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- HY-P1119
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Formyl Peptide Receptor (FPR)
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Neurological Disease
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WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide .
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- HY-P3557A
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- HY-101368
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- HY-120928
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- HY-135500
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Endothelin Receptor
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Endocrinology
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ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .
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- HY-123617
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- HY-P1196
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- HY-P1663
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VEGFR
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Others
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ATWLPPR Peptide is a biological active peptide. (This peptide is a specific VEGFR2/KDR heptapeptide antagonist, it binds VEGFR2 (KDR/flk), completely inhibiting VEGF binding to KDR and preventing VEGF-induced angiogenesis in-vivo. It specifically inhibits human endothelial cell proliferation in-vitro and totally abolishes VEGF-induced angiogenesis in-vivo.)
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- HY-P1119A
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Formyl Peptide Receptor (FPR)
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Neurological Disease
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WRW4 TFA, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 TFA specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide .
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- HY-161401
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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PAR4 antagonist 2 (Compound 31) is a protease activated receptor 4 (PAR4) antagonist, with IC50 values of 95 nM and 367 nM for human PAR4 and mouse PAR4. PAR4 antagonist 2 is active against PAR4 activation by the native protease thrombin cleavage but not the synthetic PAR4 agonist peptide AYPGKF .
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- HY-W010922
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Amino Acid Derivatives
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Others
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Fmoc-Dap(Boc)-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bicyclic peptide tachykinin NK2 antagonists .
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- HY-P3213
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![Dp[Tyr(methyl)2,Arg8]-Vasopressin](//file.medchemexpress.eu/product_pic/hy-p3213.gif)
- HY-19214
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- HY-115974
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Bombesin Receptor
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Cancer
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GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis, with anticancer activity .
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- HY-P2264
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Ephrin Receptor
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Inflammation/Immunology
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KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .
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- HY-P1271A
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nAChR
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Cardiovascular Disease
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Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
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- HY-P11052
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HSP
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Cancer
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A8 peptide is a Hsp72 antagonist. A8 peptide inhibits tumor progression and metastasis as well as enhances the cancer cells' sensitivity to apoptosis induced by chemotherapeutic agents (such as Cisplatin (HY-17394)) by blocking the Hsp72-TLR2 interaction and the subsequent activation of MDSCs. A8 peptide can be used for cancers research .
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- HY-16711
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- HY-P1196A
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- HY-120261
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- HY-17446
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HOE 140
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Bradykinin Receptor
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Endocrinology
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Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively .
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- HY-109022
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MK-8031; AGN-241689
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CGRP Receptor
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Neurological Disease
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Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine .
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- HY-108896
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HOE 140 acetate
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Bradykinin Receptor
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Inflammation/Immunology
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Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC50 and Ki of 1.07 nM and 0.798 nM respectively .
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- HY-125075
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Bombesin Receptor
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PD 165929 is a high affinity and competitive non-peptide neuromedin-B (NMB) receptor selective antagonist (Ki: 6.3 nM; IC50: 150 nM for rat NMB receptor) .
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- HY-13222
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Opioid Receptor
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Neurological Disease
Cancer
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BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic .
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- HY-P3212
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Neuropeptide Y Receptor
Others
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Cancer
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Allo-aca, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca blocks leptin signaling and action in numerous in vitro and in vivo models .
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- HY-107533
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GnRH Receptor
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Endocrinology
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T-98475 (Compound 26d) is a potent, orally active, non-peptide luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.2 nM .
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- HY-117819
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ROR
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Inflammation/Immunology
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TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM .
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- HY-107723A
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Neuropeptide Y Receptor
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Metabolic Disease
|
|
CGP 71683 Free base serves as a powerful and highly selective non-peptide antagonist targeting the NPY Y(5) receptor, making it a valuable tool in obesity research.
|
-
- HY-101986C
-
|
AR-H 053591 dihydrochloride
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BIIE-0246 dihydrochloride (AR-H 053591 dihydrochloride) is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 value of 15 nM .
|
-
- HY-15498
-
|
BMS-927711; BHV-3000
|
CGRP Receptor
|
Neurological Disease
|
|
Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor .
|
-
- HY-18347A
-
-
- HY-W013154
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-Tic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as the biotinylated derivative of the opioid receptor antagonist TIPP .
|
-
- HY-103357
-
-
- HY-116066
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
YM471 free base is a non-peptide antagonist of vasopressin V1A and V2 receptors with potent and persistent antagonistic activity. YM471 exhibits high affinity for rat V1A and V2 receptors with K values of 0.16 and 0.77 nM, respectively .
|
-
- HY-32709
-
|
MK-0974
|
CGRP Receptor
|
Neurological Disease
|
|
Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
|
-
- HY-P0062
-
-
- HY-15498A
-
|
BMS-927711 sulfate hydrate; BHV-3000 sulfate hydrate
|
CGRP Receptor
|
Neurological Disease
|
|
Rimegepant (sulfate hydrate) is an orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM. Rimegepant (sulfate hydrate) can be used in migraine related research .
|
-
- HY-108479
-
|
SR140333
|
Neurokinin Receptor
|
Neurological Disease
|
|
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
|
-
- HY-P0062B
-
-
- HY-P1242
-
-
- HY-P1454B
-
|
|
Wnt
|
Cancer
|
|
Fz7-21S is a negative control of Fz7-21. Fz7-21 is a potent peptide antagonist of FZD7 receptors .
|
-
- HY-P0107
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
-
- HY-N8152
-
-
- HY-P3212A
-
|
|
Neuropeptide Y Receptor
|
Cancer
|
|
Allo-aca TFA, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca TFA blocks leptin signaling and action in numerous in vitro and in vivo models .
|
-
- HY-114574
-
|
|
CGRP Receptor
|
Neurological Disease
|
|
BMS-694153 is a potent antagonist of the human calcitonin gene-related peptide receptor (CGRP Receptor). BMS-694153 can be used for migraine with rapid and efficient intranasal exposure .
|
-
- HY-P1242A
-
-
- HY-113730
-
|
|
CXCR
|
Others
|
|
VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.
|
-
- HY-108483
-
|
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .
|
-
- HY-13222A
-
|
|
Opioid Receptor
|
Cancer
|
|
BAN ORL 24 free base is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 free base has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 free base can be used for the research of cancer and analgesic .
|
-
- HY-123499
-
|
|
Somatostatin Receptor
|
Cardiovascular Disease
|
|
SRA880 is a non-peptide and selective somatostatin sst(1) receptor antagonist. SRA880 exhibits antidepressant-like effects when in combination with Imipramine (HY-B1490A) .
|
-
- HY-109093
-
|
KLH-2109; OBE-2109
|
GnRH Receptor
|
Inflammation/Immunology
Cancer
|
|
Linzagolix (KLH-2109; OBE-2109) is a potent, non-peptide, and orally active GnRH antagonist. Linzagolix can be used for uterine fibroids, endometriosis, adenomyosis research .
|
-
- HY-N2600R
-
|
|
Reference Standards
Bombesin Receptor
|
Cancer
|
|
Kuwanon H (Standard) is the analytical standard of Kuwanon H. This product is intended for research and analytical applications. Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells .
|
-
- HY-P1141
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1(9-36)amide is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide acts as an antagonist to the human pancreatic GLP-1 receptor .
|
-
- HY-P2497
-
|
|
GCGR
|
Neurological Disease
|
|
Exendin (5-39) is a potent glucagon-like peptide 1 (GLP-1) receptor antagonist. Exendin (5-39) improves memory impairment in β-amyloid protein-treated rats .
|
-
- HY-P11352
-
|
RM26
|
Bombesin Receptor
|
Cancer
|
|
JMV594 (Compound RM 26) is a bombesin analogue with high affinity and antagonistic effect for gastrin releasing peptide receptor (GRPR).JMV594 can be used for the research of cancer, such as Prostate cancer .
|
-
- HY-P0062A
-
-
- HY-14184
-
-
- HY-19947
-
|
Glucagon receptor antagonists-4
|
GCGR
|
Metabolic Disease
|
|
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM) .
|
-
- HY-P1141A
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1(9-36)amide TFA is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide TFA acts as an antagonist to the human pancreatic GLP-1 receptor .
|
-
- HY-P0264A
-
|
Avexitide acetate
|
GLP Receptor
|
Metabolic Disease
|
|
Exendin(9-39) amide (Avexitide) acetate is a glucagon-like peptide-1 (GLP-1) antagonist that competes with endogenous GLP-1 for the GLP-1R, counteracting the effects of excessive GLP-1 secretion. Exendin(9-39) amide acetate can be utilized in Postbariatric hypoglycemia (PBH) research .
|
-
- HY-P0264
-
|
Avexitide
|
GLP Receptor
|
Metabolic Disease
|
|
Exendin(9-39) amide (Avexitide) is a glucagon-like peptide-1 (GLP-1) antagonist that competes with endogenous GLP-1 for binding to GLP-1 receptors, thereby antagonizing the effects of excess GLP-1 secretion. Exendin(9-39) amide can be used to study postoperative hypoglycemia (PBH) .
|
-
- HY-P0107A
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
-
- HY-P1471
-
|
22-52-Adrenomedullin (human)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
|
-
- HY-125053A
-
|
|
Glycoprotein VI
|
Cardiovascular Disease
|
|
Batifiban TFA, a cyclic peptide, is an antagonist of platelet glycoprotein GPⅡb/Ⅲa and inhibits platelet aggregation. Batifiban blocks the binding of circulating vitronectin to integrin ανβ3 .
|
-
- HY-134992
-
|
Zavegepant; BHV-3500
|
CGRP Receptor
|
Neurological Disease
|
|
Vazegepant (Zavegepant) is an orally active calcitonin gene-related peptide CGRP receptor antagonist with potential for acute research in migraine, can be administered intranasally. CGRP is an important trigger in migraine pathophysiology .
|
-
- HY-P1277
-
-
- HY-P1868
-
|
DGEA peptide
|
Integrin
|
Infection
|
|
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors .
|
-
- HY-P0211
-
|
|
GCGR
|
Cardiovascular Disease
|
|
[Ac-Tyr1,D-Phe2]GRF 1-29, amide (human), a growth hormone releasing factor (GRF) analogue, is a vasoactive intestinal peptide (VIP) antagonist .
|
-
![[Ac-Tyr1,D-Phe2]GRF 1-29, amide (human)](//file.medchemexpress.eu/product_pic/hy-p0211.gif)
- HY-114452A
-
|
BTRX-246040 tartrate
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models .
|
-
- HY-P1868A
-
|
DGEA peptide TFA
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors .
|
-
- HY-P1277A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively .
|
-
- HY-P10474
-
|
|
Drug Isomer
|
Others
|
|
RYTVELA is a deriviative of the peptide antagonist of interleukin-1 receptor 1 (IL-1R1) d-(RYTVELA) (HY-P10353) that contains all L-amino acids .
|
-
- HY-19529
-
-
- HY-W041989
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-Oic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as [desArg 10]HOE 140, which has bradykinin B1 antagonist activity .
|
-
- HY-111214
-
-
- HY-P1050
-
COG 133
2 Publications Verification
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
COG 133 is a fragment of Apolipoprotein E (APOE) peptide. COG 133 competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC50 of 445 nM .
|
-
- HY-P4127A
-
-
- HY-14184A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
|
-
- HY-W013153
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-D-Tic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as [desArg 10]HOE 140, which has bradykinin B1 antagonist activity .
|
-
- HY-P1327
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BVD 10, a neuropeptide Y (NPY) analogue peptide, is a highly selective NPY Y1 receptor antagonist. BVD10 significantly prevents NPY-induced glutamate increase. BVD 10 can be used for seizure research .
|
-
- HY-12080
-
|
ZK-811752
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-P10102
-
Kp7-6
2 Publications Verification
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Kp7-6, a Fas mimetic peptide, is a Fas/FasL antagonist. Kp7-6 protects cells from Fas-mediated apoptosis, and protects mice from Fas-mediated hepatic injury .
|
-
- HY-70068
-
-
- HY-117670
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
PD-161182 is a non-peptide NK-3 antagonist. PD-161182 can be studied in NK-3-related central nervous system disturbances, pain, inflammation, pulmonary and skin diseases .
|
-
- HY-117971
-
|
|
CXCR
Formyl Peptide Receptor (FPR)
|
Others
|
|
BVT173187 is a selective inhibitor of the neutrophil formyl peptide receptor FPR1, with activity that inhibits FPR1 activation. BVT173187 inhibits FPR1 agonist-induced activation in neutrophils, reduces adhesion molecule mobilization and superoxide anion production, and has inhibitory activity on FPR1 similar to that of earlier described peptide antagonists, but also has effects on C5aR and CXCR signaling.
|
-
- HY-P5891
-
|
|
PKC
|
Cardiovascular Disease
|
|
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
|
-
- HY-14184S
-
-
- HY-12080A
-
|
ZK-811752 hydrochloride
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-W006937
-
|
Boc-p-amino-D-Phe(Fmoc)-OH; Boc-D-phe(4-NH-fmoc)-OH
|
Amino Acid Derivatives
|
Others
|
|
Boc-D-(4-fmoc)-aminophenylalanine (Boc-p-amino-D-Phe(Fmoc)-OH) is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize peptides with gonadotropin-releasing hormone antagonist activity .
|
-
- HY-116854
-
|
|
GCGR
|
Metabolic Disease
|
|
NNC 92-1687 is a non-peptide competitive human glucagon receptor antagonist (IC50=20 μM; Ki=9.1 μM). NNC 92-1687 can be used in the research of type 2 diabetes .
|
-
- HY-120308
-
|
SR140603
|
Neurokinin Receptor
|
Neurological Disease
|
|
(R)-Nolpitantium is the R-enantiomer of Nolpitantium (HY-108479). Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
|
-
- HY-P10388
-
|
|
CD47
TGF-β Receptor
|
Cancer
|
|
TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
|
-
- HY-167688
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
GSK-1562590 is a uropeptide-II receptor antagonist with high affinity and selectivity. GSK-1562590 exhibits significant antagonistic activity in multiple bioassays and, in contrast, displays relatively sustained receptor binding times. GSK-1562590 can inhibit human urinary peptide-II-induced aortic contraction in rats in experiments, and its effect can last for at least 24 hours .
|
-
- HY-P1285
-
|
Con-R
|
iGluR
|
Neurological Disease
|
|
Conantokin R (Con-R) is an NMDA receptor peptide antagonist with an IC50 of 93 nM. Conantokin R binds Zn 2+ and Mg 2+ with Kds of 0.15 μM and 6.5 μM, respectively. Conantokin R shows anticonvulsant activity .
|
-
- HY-17446R
-
|
HOE 140 (Standard)
|
Reference Standards
Bradykinin Receptor
|
Endocrinology
|
|
Icatibant (Standard) is the analytical standard of Icatibant. This product is intended for research and analytical applications. Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively .
|
-
- HY-108896R
-
|
HOE 140 acetate (Standard)
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
Icatibant (acetate) (Standard) is the analytical standard of Icatibant (acetate). This product is intended for research and analytical applications. Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC50 and Ki of 1.07 nM and 0.798 nM respectively .
|
-
- HY-19431
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM) .
|
-
- HY-W370556
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
(Rac)-LM11A-31 is a racemate of LM11A-31. LM11A-31 is a non-peptide modulator of p75NTR (neurotrophin receptor p75) and is an orally effective proNGF antagonist .
|
-
- HY-17012
-
|
RPR 100893
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Dapitant (RPR 100893) is a non-peptide Substance P antagonist with high affinity for the human NK1 receptor. It belongs to the 7,7,4-trimethylperhydroisoindole class of compounds. Dapitant inhibits the binding of Substance P to NK1 receptors, thereby blocking its neurokinin-mediated effects. This novel antagonist represents a potential therapeutic option for conditions involving Substance P, such as neurogenic inflammation and pain modulation .
|
-
- HY-P1050A
-
|
|
Apolipoprotein
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM .
|
-
- HY-P6292
-
|
|
PACAP Receptor
|
Neurological Disease
|
|
KS-133 is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 plays an important role in schizophrenia research .
|
-
- HY-18347AR
-
|
YM 087 (Standard)
|
Reference Standards
Vasopressin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Conivaptan (hydrochloride) (Standard) is the analytical standard of Conivaptan (hydrochloride). This product is intended for research and analytical applications. Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.
|
-
- HY-P3117
-
|
Pituitary adenylate cyclase-activating peptide (6-27)
|
Adenylate Cyclase
|
Neurological Disease
|
|
PACAP (6-27) (human, ovine, rat) is a PACAP receptor antagonist that blocks the canine adrenal catecholamine response to exogenous vasoactive intestinal peptide (VIP). PACAP (6-27) (human, ovine, rat) has the potential to study cardiovascular and neurological diseases .
|
-
- HY-P10465
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain .
|
-
- HY-P5327
-
|
|
Bcl-2 Family
|
Others
|
|
r8 Bid BH3 is a biological active peptide. (The Bid BH3 is a pro-apoptotic member of the 'BH3-only' subset of BCL-2 family proteins that constitute a critical control point in apoptosis. r8BIDBH3 is lethal to human leukemia cell lines that expresse Bcl-2. The Bcl-2 antagonists may have the potential to be efficacious in cancer therapy. Poly-D-arginine (d-isomer as denoted by rrrrrrrr) is fused to the Bid BH3 peptide to facilitate cellular uptake of the peptide.)
|
-
- HY-U00235
-
|
|
Integrin
|
Inflammation/Immunology
|
|
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
|
-
- HY-P991415
-
|
AM712
|
VEGFR
Tie
|
Others
|
|
ASKG-712 (AM712) is a recombinant anti-VEGF humanized monoclonal antibody and Ang-2 antagonist peptide fusion protein. ASKG-712 can be used in Wet age-related macular degeneration and Diabetic macular oedema research .
|
-
- HY-14369
-
-
- HY-P4776
-
-
- HY-10049A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
CP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide neurokinin NK1 antagonist, with a pIC50 of 9.8 for human NK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects .
|
-
- HY-P1242B
-
|
|
Drug Derivative
|
Inflammation/Immunology
|
|
NEP(1-40), N-terminal uncapped is a NEP(1-40) (HY-P1242) analog without the acetylation modification at the N-terminal. NEP(1-40) is a Nogo-66 receptor (NgR) antagonist peptide .
|
-
- HY-76612
-
-
- HY-125053
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Batifiban, a cyclic peptide, is a platelet glycoprotein GPⅡb/Ⅲa antagonist, and inhibits platelet aggregation. Batifiban blocks circulating vitronectin binding to integrin ανβ3, Batifiban can be used for research of acute coronary syndromes .
|
-
- HY-P10486
-
|
|
Bacterial
|
Infection
|
|
AIP-II is a macrocyclic peptide signaling molecule used for quorum sensing, which can be produced be Staphylococcus aureus. AIP-II binds to AgrC-II receptor, regulates the virulence gene expression in Staphylococcus aureus. AIP-II is an antagonist for AgrC-I receptor .
|
-
- HY-107080
-
|
|
Integrin
|
Cardiovascular Disease
|
|
RPR-109891 is an orally active glycoprotein IIb/IIIa peptide antagonist. RPR-109891 can decrease platelet count and reduce platelet survival time. RPR-109891 can be used for the research of cardiovascular disease, such as myocardial infarction .
|
-
- HY-14789
-
-
- HY-P3542
-
|
|
GCGR
|
Metabolic Disease
|
|
Des His1, Glu8 Exendin-4 is a potent glucagon-like peptide-1 receptor (GLP-1-R) antagonist. Des His1, Glu8 Exendin-4 improves glucose homeostasis by regulating both insulin secretion and glucose production. Des His1, Glu8 Exendin-4 can be used for the research of type 2 diabetic and gastrointestinal .
|
-
- HY-19374
-
|
|
GCGR
|
Metabolic Disease
|
|
BAY-27-9955 is an orally active non-peptide glucagon receptor antagonist. Bay 27-9955 competitively blocks the interaction of glucagon with the human glucagonreceptor at an IC50 value of 110 nM. BAY-27-9955 can be used for the study of type 2 diabetes .
|
-
- HY-108677
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent .
|
-
- HY-P1293
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
|
-
- HY-P6292A
-
|
|
PACAP Receptor
|
Neurological Disease
|
|
KS-133 TFA is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 TFA plays an important role in schizophrenia research .
|
-
- HY-P10405
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
TAT-D1 peptide is a selective D1-D2 heterogeneous antagonist. TAT-D1 peptide destroys the heterodimer of the D1-D2 receptor by interacting with the specific domain of the D2 receptor through its unique amino acid sequence, in particular the two glutamate residues at the C terminal of the D1 receptor. TAT-D1 peptide can be used to study the role of D1-D2 receptor heterodimers in the regulation of depressive and anxiety-like behaviors .
|
-
- HY-10898
-
-
- HY-106268A
-
|
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Larazotide acetate is a peptide which is an orally active zonulin antagonist. Larazotide acetate shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide acetate can be used for the research of celiac disease and infection.
|
-
- HY-P0097A
-
|
Melanostatine-5 acetate salt
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-P0097
-
|
Melanostatine-5
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-P1419
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
AP 811 is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 displays >20000-fold selectivity for NPR3 over NPR1. AP 811 abolishes ANP-induced pump stimulation .
|
-
- HY-P0102
-
|
|
mAChR
|
Endocrinology
|
|
Dipeptide diaminobutyroyl benzylamide diacetate, a Wagerlin-1-mimicking peptide, is a mAChR antagonist. Dipeptide diaminobutyroyl benzylamide diacetate can induce muscle relaxation. Dipeptide diaminobutyroyl benzylamide diacetate can be used in the research of skin aging, especially facial wrinkles (such as crow's feet and wrinkles around the eyes) .
|
-
- HY-110155A
-
|
|
Drug Isomer
|
Neurological Disease
|
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist .
|
-
- HY-P1419A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
AP 811 acetate is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 acetate displays >20000-fold selectivity for NPR3 over NPR1. AP 811 acetate abolishes ANP-induced pump stimulation .
|
-
- HY-164535
-
|
AMG 133
|
Antibody-Drug Conjugates (ADCs)
GLP Receptor
|
Metabolic Disease
|
|
Maridebart cafraglutide (AMG 133) is an antibody-peptide conjugate acting as a GLP-1 receptor agonist and an antagonist of the GIP receptor. Maridebart cafraglutide reduces body weight and improve metabolic markers in male obese mice and cynomolgus monkeys. Maridebart cafraglutide is promising for research of obesity .
|
-
- HY-124767
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
SR 142948A is a non-peptide neuropeptide neuropeptin (NT) receptor antagonist. SR 142948A is able to bind to neuropeptin receptors, especially with high affinity for NT1 and NT2 receptors. SR 142948A is mainly used to study the role of neuropeptide in the neurotransmitter system, especially the dopamine system .
|
-
- HY-14184R
-
|
ACT-064992 (Standard)
|
Reference Standards
Endothelin Receptor
Apoptosis
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .
|
-
- HY-P3429
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-P1143
-
|
|
GCGR
|
Metabolic Disease
|
|
[Des-His1,Glu9]-Glucagon amide is a potent and peptide antagonist of the glucagon receptor, with a pA2 of 7.2. [Des-His1,Glu9]-Glucagon amide is potentially useful in the study of the pathogenesis of diabetes .
|
-
![[Des-His1,Glu9]-Glucagon amide](//file.medchemexpress.eu/product_pic/hy-p1143.gif)
- HY-P1471A
-
|
22-52-Adrenomedullin (human) (TFA)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
|
-
- HY-P1293A
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
-
- HY-32709S
-
|
MK-0974-d8
|
Isotope-Labeled Compounds
CGRP Receptor
|
Neurological Disease
|
|
Telcagepant-d8 (MK-0974-d8) is deuterium labeled Telcagepant. Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
|
-
- HY-106268
-
|
|
Gap Junction Protein
|
Infection
Inflammation/Immunology
|
|
Larazotideis a peptide which is an orally active zonulin antagonist. Larazotide shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide can be used for the research of celiac disease and infection .
|
-
- HY-P1651
-
SOR-C13
1 Publications Verification
|
TRP Channel
|
Cancer
|
|
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity .
|
-
- HY-P5645
-
LEAP-2
1 Publications Verification
Human liver expressed antimicrobial peptide-2
|
GHSR
Interleukin Related
IFNAR
TNF Receptor
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
LEAP-2 (Human liver expressed antimicrobial peptide-2) is a GHS-R1a antagonist, with an IC50 of 6.0 nM. LEAP-2 suppresses the orexigenic effect of ghrelin. LEAP-2 attenuates ghrelin-induced growth hormone (GH) release and reduces basal food intake. LEAP-2 exhibits antimicrobial activity against microbial model organisms. LEAP-2 can be used for the study of obesity and infection .
|
-
- HY-125373
-
|
|
Integrin
|
Cardiovascular Disease
|
|
L-767685, the ethyl ester prodrug of L-767679 (HY-116925), is a non-peptide glycoprotein IIb/IIIa receptor (GPIIb-IIIa receptor) antagonist. L-767679 has a potent anti-platelet aggregation effect. L-767685 can be used for research on antithrombosis .
|
-
- HY-P4072
-
|
|
PD-1/PD-L1
|
Cancer
|
|
(D)-PPA 1 is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy .
|
-
- HY-108625
-
SHA 68
1 Publications Verification
|
Neuropeptide S Receptor
|
Neurological Disease
|
|
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
|
-
- HY-10119
-
|
SCH 530348
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-106840A
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Metabolic Disease
|
|
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .
|
-
- HY-129296
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
YM-44781 free acid is a non-peptide neuropeptide receptor antagonist with efficient NK(2) and NK(1) receptor antagonist activity. YM-44781 exhibits significant binding affinity on the NK(2) receptor (pKi = 9.94) and also on the NK(1) receptor Higher binding affinity (pKi = 9.09). In addition, YM-44781 also showed significant inhibitory effects on bladder contraction induced by selective NK(1) receptor agonists .
|
-
- HY-116216
-
|
|
Bombesin Receptor
|
Cancer
|
|
PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM . PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist . PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively .
|
-
- HY-108055
-
|
|
Urotensin Receptor
Others
|
Cardiovascular Disease
|
|
Urantide is a selective and competitive urotensin-II (UT) receptor antagonist peptide (pKB=8.3) that blocks human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide can be used to study the (patho)physiological role of hU-II in the mammalian cardiovascular system .
|
-
- HY-P1651A
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity .
|
-
- HY-10657
-
|
|
Urotensin Receptor
|
Cardiovascular Disease
Others
|
|
SB-706375 is an antagonist of the Urotensin II (UII) receptor. By blocking the Urotensin II receptor, SB-706375 reduces the kidney's response to UII and Urotensin-related peptide (URP) and significantly increases the Glomerular Filtration Rate (GFR). SB-706375 can be used in research on kidney diseases and hypertension .
|
-
- HY-P1143A
-
|
|
GCGR
|
Metabolic Disease
|
|
[Des-His1,Glu9]-Glucagon amide TFA is a potent and peptide antagonist of the glucagon receptor, with a pA2 of 7.2. [Des-His1,Glu9]-Glucagon amide TFA is potentially useful in the study of the pathogenesis of diabetes .
|
-
![[Des-His1,Glu9]-Glucagon amide TFA](//file.medchemexpress.eu/product_pic/hy-p1143a.gif)
- HY-10119A
-
|
SCH 530348 sulfate
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-12366
-
|
MK-1602
|
CGRP Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
|
-
- HY-P4072A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
(D)-PPA 1 TFA is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 TFA serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 TFA binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy .
|
-
- HY-P3429A
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA TFA is conjugated to the cell permeable peptide TAT47-57. SAMβA TFA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-P1309
-
-
- HY-108626
-
|
NCGC84
|
Neuropeptide S Receptor
|
Neurological Disease
|
|
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA2 of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively .
|
-
- HY-P3343A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells .
|
-
- HY-P1039
-
|
PHCVPRDLSWLDLEANMCLP
|
Raf
|
Cancer
|
|
R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1 .
|
-
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
-
- HY-P2026
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [ 125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells .
|
-
- HY-P1263
-
-
- HY-103286
-
|
|
Bombesin Receptor
|
Cancer
|
|
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
|
-
- HY-P3226
-
|
|
IGF-1R
|
Metabolic Disease
|
|
JB-1, an IGF-1 peptide analog, is a selective and potent IGF-1R antagonist. JB-1 competes with IGF-1 by binding the IGF-1 receptor. JB-1 prevents the autophosphorylation of IGF-1R, and has no activity in IGF-II .
|
-
- HY-15522
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
WAY-267464 is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
|
-
- HY-P1039A
-
|
PHCVPRDLSWLDLEANMCLP TFA
|
Raf
|
Cancer
|
|
R18 TFA is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1 .
|
-
- HY-106203A
-
|
SSR-125543 hydrochloride
|
CFTR
|
Metabolic Disease
|
|
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P1263A
-
-
- HY-106203
-
|
SSR-125543
|
CFTR
|
Metabolic Disease
|
|
Crinecerfont (SSR-125543) is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-103247B
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
EMD-66684 potassium salt is a non-peptide angiotensin II receptor antagonist that demonstrates significant antihypertensive effects in spontaneously hypertensive rats. EMD-66684 potassium salt exhibits nanomolar affinity for angiotensin II receptors, comparable to losartan in potency. EMD-66684 potassium salt shows increased activity when modified with acetamides, leading to superior blood pressure reduction.
|
-
- HY-109022A
-
|
(3R,5R,6S)-MK-8031; (3R,5R,6S)-AGN-241689
|
CGRP Receptor
|
Neurological Disease
|
|
(3R,5R,6S)-Atogepant ((3R,5R,6S)-MK-8031) is the enantiomer of Atogepant (HY-109022). Atogepant is a calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
|
-
- HY-108679
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
WAY-267464 (hydrochloride) is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 (hydrochloride) can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 (hydrochloride) can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
|
-
- HY-15011
-
|
|
Oxytocin Receptor
|
Others
|
|
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR .
|
-
- HY-70068R
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-408124 (Standard) is the analytical standard of SB-408124. This product is intended for research and analytical applications. SB-408124 is a non-peptide OX1 receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor .
|
-
- HY-B0290A
-
|
ONO-1078 hemihydrate
|
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-106203C
-
|
SSR-125543 tosylate
|
CFTR
|
Metabolic Disease
|
|
Crinecerfont tosylate (SSR-125543 tosylate) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont tosylate can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont tosylate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B0290
-
-
- HY-P7061A
-
|
|
Apelin Receptor (APJ)
CXCR
|
Infection
Endocrinology
|
|
ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
|
-
- HY-P10135
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
RES-701-1 is a cyclic peptide composed of 16 common L-amino acids, acting as a specific antagonist for the ETB receptor. RES-701-1 can inhibit the binding of 125I-ET-1 (125I-labeled Endothelin (ET)-1) to the ETB receptor, with an IC50 value of 10 nM .
|
-
- HY-P1795
-
|
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
Boc-dPhe-Leu-dPhe-Leu-Phe (Boc-fLfLF) is a selective N-formyl peptide receptor1 (FPR1) antagonist. Boc-dPhe-Leu-dPhe-Leu-Phe inhibits fMIFL(HY-P0224)-induced NADPH oxidase activity. Boc-dPhe-Leu-dPhe-Leu-Phe can be used for the study of inflammation .
|
-
- HY-14789R
-
|
|
GnRH Receptor
Nuclear Factor of activated T Cells (NFAT)
|
Endocrinology
Cancer
|
|
(R)-Elagolix (Standard) is the analytical standard of (R)-Elagolix. This product is intended for research and analytical applications. Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
|
-
- HY-P7061
-
|
|
CXCR
Apelin Receptor (APJ)
|
Infection
Endocrinology
|
|
ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
|
-
- HY-117952
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L 743310 is a non-peptide, selective antagonist of the human neurokinin hNK1 receptor, with high affinity for primate and cloned human hNK1 receptors and lower affinity for rodent NK1 receptors. L 743310 inhibits resiniferatoxin-induced plasma protein extravasation in guinea pig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis .
|
-
- HY-P1309A
-
|
PAR-4-AP TFA; AY-NH2 TFA
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist .
|
-
- HY-118037
-
|
|
CXCR
|
Inflammation/Immunology
|
|
VUF10132 is a non-peptide CXCR3 receptor antagonist with anti-inflammatory activity, inhibiting diseases such as rheumatoid arthritis, multiple sclerosis, and psoriasis. VUF10132 has high affinity for the human CXCR3 receptor but slightly lower affinity for the murine CXCR3 receptor. Additionally, VUF10132 exhibits inverse agonist properties at the CXCR3 receptor .
|
-
- HY-107692
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit .
|
-
- HY-P10831
-
|
|
VEGFR
|
Cardiovascular Disease
Cancer
|
|
GNQWFI, an anti-Flt1 peptide, is a VEGFR1-specific antagonist. GNQWFI blocks the interaction of VEGFR1 with various VEGFR1 ligands, such as VEGFA, VEGFB, and placental growth factor (PIGF) and inhibits VEGF-induced endothelial cell migration and tube formation. GNQWFI is promising for research of cancer, asthma, and other ocular diseases .
|
-
- HY-P1159
-
-
![[D-p-Cl-Phe6,Leu17]-VIP](//file.medchemexpress.eu/product_pic/hy-p1159.gif)
- HY-123460
-
|
|
Somatostatin Receptor
|
Cancer
|
|
BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst3 receptor (Ki=0.92 nM). In addition, BN-81674 reversed the inhibition of cyclic AMP accumulation induced by 1 nM somatostatin through the sst3 receptor with an IC50 value of 0.84 nM. BN-81674 can be used in cancer research .
|
-
- HY-Y0265
-
|
Indoline-2,3-dione
|
Monoamine Oxidase
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
|
-
- HY-76612R
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-408124 (Hydrochloride) (Standard) is the analytical standard of SB-408124 (Hydrochloride). This product is intended for research and analytical applications. SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor .
|
-
- HY-110166
-
|
|
Trk Receptor
|
Neurological Disease
|
|
PD 90780 is a non peptide antagonist of nerve growth factor (NGF). PD 90780 interacts with NGF, prevents NGF binds with p75 NTR. PD 90780 inhibits NGF-p75 NTR interaction with IC50s of 23.1 and 1.8 μM in PC12 cells and PC12 nnr5 cells, respectively .
|
-
- HY-P1159A
-
|
|
PACAP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
[D-p-Cl-Phe6,Leu17]-VIP TFA is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC50 of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP TFA has no activity on glucagon, secretin or GRF receptors .
|
-
![[D-p-Cl-Phe6,Leu17]-VIP TFA](//file.medchemexpress.eu/product_pic/hy-p1159a.gif)
- HY-P3608
-
|
|
GCGR
|
Metabolic Disease
|
|
[Des-His1,Glu9] Glucagon is a potent glucagon receptor system peptide antagonist. [Des-His1,Glu9] Glucagon enhances the glucose-stimulated release of insulin from pancreatic islet cells. [Des-His1,Glu9] Glucagon can be used to research diabetes .
|
-
![[Des-His1,Glu9] Glucagon](//file.medchemexpress.eu/product_pic/hy-p3608.gif)
- HY-W751574
-
-
- HY-103377
-
|
|
CRFR
|
Inflammation/Immunology
Endocrinology
|
|
Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome .
|
-
- HY-N2359
-
|
|
Beta-lactamase
PKC
Bcl-2 Family
Apoptosis
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM . Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity . Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy .
|
-
- HY-138106
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-D-Cit-OH is citrulline with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as H-Dmt-D-Cit-Aba-b-Ala-NMe-30,50-(CF3)2-Bn and H-Dmt-D-Cit-Aba-b-Ala-NMe-Bn with neurokinin-1 antagonist activity .
|
-
- HY-10119R
-
|
SCH 530348 (Standard)
|
Reference Standards
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-106840
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Metabolic Disease
|
|
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .
|
-
- HY-10119S
-
|
SCH 530348-d5
|
Protease Activated Receptor (PAR)
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-P10896
-
|
|
Bombesin Receptor
|
Cancer
|
|
NOTA-P2-RM26 is an antagonist of Bombesin (HY-P0195) analogs, and the gastrin-releasing peptide receptor (GRPR/BB2) is a molecular target for prostate cancer visualization. NOTA-P2-RM26 is labeled with 111In and 68Ga for prostate cancer imaging studies using PET and SPECT/CT .
|
-
- HY-100383
-
|
BHI1
|
Bcl-2 Family
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
|
-
- HY-12366R
-
|
MK-1602 (Standard)
|
CGRP Receptor
Reference Standards
|
Cardiovascular Disease
Neurological Disease
|
|
Ubrogepant (Standard) is the analytical standard of Ubrogepant. This product is intended for research and analytical applications. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
|
-
- HY-106203B
-
|
(R)-SSR-125543
|
CFTR
|
Metabolic Disease
|
|
(R)-Crinecerfont is the R-enantiomer of Crinecerfont (HY-106203). Crinecerfont (SSR-125543) is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research. Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
|
-
- HY-121156
-
|
LF 16-0687; XY-2405
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases .
|
-
- HY-121156A
-
|
LF 16-0687 hydrochloride; XY-2405 hydrochloride
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .
|
-
- HY-P1812
-
AUNP-12
3 Publications Verification
NP-12
|
PD-1/PD-L1
|
Cancer
|
|
AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
-
- HY-P10373
-
|
|
JAK
IFNAR
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
pJAK2(1001-1013) is a cell-penetrating peptide that corresponds to the activation loop of JAK2 tyrosine kinase and functions as a SOCS1/3antagonist. pJAK2 (1001-1013) blocks SOCS1-mediated negative regulation of immune function, and enhances the biological activity of cytokines such as IFNγ and IL6. pJAK2(1001-1013) inhibits the replication of a broad range of viruses and exerts dose-dependent protective efficacy against lethal viral infections. pJAK2(1001-1013) can be used for the study of immune regulation and infection .
|
-
- HY-15039
-
|
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
|
-
- HY-P1812A
-
|
NP-12 TFA
|
PD-1/PD-L1
|
Cancer
|
|
AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
-
- HY-101764
-
|
SR 27897
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin .
|
-
- HY-106994A
-
|
YM598
|
Endothelin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .
|
-
- HY-B0780
-
-
- HY-10119AR
-
|
SCH 530348 sulfate (Standard)
|
Reference Standards
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (sulfate) (Standard) is the analytical standard of Vorapaxar (sulfate). This product is intended for research and analytical applications. Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-P10550
-
|
|
VEGFR
|
Cancer
|
|
VGB4 is a VEGF-A and VEGF-B antagonist peptide that duplicates two binding domains of VEGF-B (loop 1 and loop3) and are linked together by the receptor-binding domain of VEGF-A (loop3). VGB4 has significant anti-angiogenic and anti-tumor activities and can regulate tumor growth and metastasis through multiple mechanisms. VGB4 could be used in anti-tumor research .
|
-
- HY-167686
-
|
Homopisatin
|
Integrin
|
Cardiovascular Disease
|
|
Variabilin (Homopisatin) is a potent RGD-containing antagonist of glycoprotein IIb-IIIa and platelet aggregation inhibitor from the hard tick Dermacentor variabilis. Variabilin potently inhibits platelet aggregation induced by the platelet agonists ADP, collagen, and thrombin receptor peptide SFLLRNP. Variabilin also blocks platelet adhesion to immobilized Fg. In addition, Variabilin inhibits binding of purified human GPIIb-IIIa to immobilized Fg .
|
-
- HY-108625R
-
|
|
Neuropeptide S Receptor
|
Neurological Disease
|
|
SHA 68 (Standard) is the analytical standard of SHA 68. This product is intended for research and analytical applications. SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
|
-
- HY-B0290S1
-
-
- HY-B0290AR
-
|
|
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pranlukast (hemihydrate) (Standard) is the analytical standard of Pranlukast (hemihydrate). This product is intended for research and analytical applications. Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-P1617
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
LY 190388 is a penicillamine-containing enkefa peptide analog with μ receptor agonist activity. LY 190388 showed analgesic effect in inhibiting the writhing response in mice after intracerebroventricular administration. The analgesic effect of LY 190388 is not caused by its δ receptor agonist action, but by its μ receptor agonist activity. When LY 190388 is used together with the δ receptor antagonist ICI 174864, an additive analgesic effect is produced .
|
-
- HY-106994
-
|
YM598 free base
|
Endothelin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .
|
-
- HY-113918
-
|
|
PTHR
|
Metabolic Disease
|
|
SW-106 is a parathyroid hormone receptor 1 (PTHR1) antagonist. SW106 antagonizes PTHR1-mediated cAMP signaling induced by the peptide analog, M-PTH (1-11), as well as by the native PTH (1-9) sequence, as tethered to the extracellular end of transmembrane domain (TMD) helix-1 of the receptor. SW-106 can be used for the research of metabolic disease .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-10805A
-
|
ACT 078573 hydrochloride
|
Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca 2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
|
-
- HY-B0290R
-
|
ONO-1078 (Standard)
|
Reference Standards
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pranlukast (Standard) is the analytical standard of Pranlukast. This product is intended for research and analytical applications. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-P2025
-
|
|
Histone Methyltransferase
|
Neurological Disease
|
|
JMV 236 is a cholecystokinin antagonist with appetite-suppressing activity. JMV 236 affects the regulation of food intake through the interaction of the intestinal endogenous peptide PrRP and the CCK1 receptor. The administration of JMV 236 activates PrRP neurons located in the NTS, thereby enhancing its appetite-suppressing effect. JMV 236 has significant effects on areas of the central nervous system associated with food intake, especially during states of starvation .
|
-
- HY-10805
-
|
ACT 078573
|
Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca 2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-103277A
-
|
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
|
BIM 23042 TFA, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin?B?(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
|
-
- HY-103277
-
|
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
|
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin?B?(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
|
-
- HY-12366S
-
|
MK-1602-d5
|
Isotope-Labeled Compounds
CGRP Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
|
-
- HY-P5765
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galanin (1-13)-spantide I is a chimeric peptide composed of the N-terminal fragment of galanin (amino acids 1-13) and spantide, a known substance P receptor antagonist. Galanin (1-13)-spantide I has a high affinity for spinal galanin receptor (Kd=1.16 nM). Galanin (1-13)-spantide I can be used to study the effects of galanin on feeding behavior .
|
-
- HY-W394903R
-
|
|
Reference Standards
JAK
Drug Metabolite
|
Cancer
|
|
Isatin (Standard) is the analytical standard of Isatin. This product is intended for research and analytical applications. Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
|
-
- HY-19347
-
|
WD-Repeat Protein 5-0103
|
WDR5
|
Neurological Disease
Cancer
|
|
WDR5-0103 (WD-Repeat Protein 5-0103) is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with a Kd of 450 nM. WDR5-0103 competitively binds to the peptide-binding pocket of WDR5, blocking the interaction between WDR5 and mixed-lineage leukemia (MLL) protein and inhibiting the methyltransferase activity of MLL. WDR5-0103 is mainly used in the research of cancer and neurodegenerative diseases .
|
-
- HY-103377R
-
|
|
Reference Standards
CRFR
|
Inflammation/Immunology
Endocrinology
|
|
Antalarmin (hydrochloride) (Standard) is the analytical standard of Antalarmin (hydrochloride). This product is intended for research and analytical applications. Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome .
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- HY-Y0265R
-
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Indoline-2,3-dione (Standard)
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Reference Standards
Monoamine Oxidase
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Isatin (Standard) is the analytical standard of Isatin. This product is intended for research and analytical applications. Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
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- HY-118918
-
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Vasopressin Receptor
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Endocrinology
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|
YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for rat liver V1A receptors with a Ki value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with Ki values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease .
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- HY-P2380
-
|
TFRGAP
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
PAR3 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 1 (PAR1) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR3 and residues 39-44 of the full-length human sequence. PAR3 (1-6) activates p42/44 MAPK signaling in fibroblasts expressing PAR1, but not PAR3, an effect that can be blocked by the PAR1 antagonist RWJ 56110.
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- HY-16992A
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W-54011
5 Publications Verification
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Complement System
Reactive Oxygen Species (ROS)
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Inflammation/Immunology
|
|
W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively .
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- HY-101283
-
HCH6-1
5 Publications Verification
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Formyl Peptide Receptor (FPR)
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Inflammation/Immunology
|
|
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases .
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- HY-117053
-
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Neurokinin Receptor
|
Neurological Disease
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|
ZM 253270 is a species-selective non-peptide NK-2 receptor (NK-2R) antagonist. ZM 253270 competitively inhibits the binding of [ 3H]NKA to native or cloned NK-2R from hamster bladder (Ki=2 nM), but has a weaker inhibitory effect (48-fold) on the binding of [ 3H]NKA to cloned human NK-2R .
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- HY-P0262
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
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|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM) .
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- HY-107732
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors .
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- HY-P1454
-
Fz7-21
3 Publications Verification
Ac-LPSDDLEFWCHVMY-NH2
|
Wnt
|
Cancer
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|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs the function of FZD7 in Wnt–β-catenin signalling and stem cell function in intestinal organoids .
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-
- HY-107691
-
|
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Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
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|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
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-
- HY-110155
-
|
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Neurotensin Receptor
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
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-
- HY-P1454A
-
|
Ac-LPSDDLEFWCHVMY-NH2 TFA
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Wnt
|
Cancer
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|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 TFA impairs the function of FZD7 in Wnt-β-catenin signalling and stem cell function in intestinal organoids .
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- HY-P0039
-
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Bombesin Receptor
|
Cancer
|
|
BIM-26226 is a selective gastrin-releasing peptide receptor (GRPR) (IC50 = 6 nM) and bombesin receptor (BN receptor) antagonist. BIM-26226 antagonizes BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 is specific for the GRP-preferring BN receptor subtype with no interference with GRP receptor system. BIM-26226 can induce the synthesis of somatostatin receptor but has no significant effect on tumor growth .
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- HY-10805R
-
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Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Almorexant (Standard) is the analytical standard of Almorexant. This product is intended for research and analytical applications. Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
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- HY-117088
-
|
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Neurokinin Receptor
|
Neurological Disease
|
|
LM11A-31, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
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- HY-120767
-
|
KLH-2109 choline; OBE-2109 choline
|
GnRH Receptor
|
Inflammation/Immunology
Cancer
|
|
Linzagolix choline (KLH-2109 choline) is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist with oral activity. Linzagolix choline inhibits the release of endogenous gonadotropins such as luteinizing hormone LH and follicle-stimulating hormone FSH by binding to the GnRH receptor within the pituitary gland. This inhibition results in a reduction in the production of sex hormones such as estrogen and progesterone, which in turn affects the course of sex hormone-dependent diseases. Linzagolix choline can be used in the study of sex hormone-dependent diseases such as endometriosis and uterine fibroids .
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- HY-123864
-
|
S 448
|
Integrin
|
Cardiovascular Disease
Cancer
|
|
SC-68448 (S 448) is a selective αvβ3 antagonist (IC50 = 1 nM). SC-68448 inhibits αvβ3-mediated endothelial cell proliferation. SC-68448 reduces the total level of αvβ6 in NHBE cells. SC-68448 inhibits angiogenesis in a rat corneal neoplasia model. SC-68448 inhibits tumor growth and completely prevents the development of hypercalcemia in a rat Ledich cell tumor model. SC-68448 can be used in research on cardiovascular and cerebrovascular diseases such as hypercalcemia and cancers such as testicular interstitial cell tumors .
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- HY-P1681
-
|
|
Sodium Channel
|
Neurological Disease
|
|
GpTx-1 is a peptide-based NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 demonstrates potent inhibitory activity against the NaV1.7 channel with an IC50 value of 10 nM, while exhibiting excellent selectivity for NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .
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- HY-P1681A
-
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|
Sodium Channel
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Neurological Disease
|
|
GpTx-1 TFA is a peptide-based NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the NaV1.7 channel with an IC50 value of 10 nM, while exhibiting excellent selectivity for NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .
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-
- HY-123244
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
YC137 is a potent Bcl-2 antagonist with Kis of 1.3 μM and >100 μM for Bcl-2 and Bcl-xL when assayed in Bis-Tris buffer, respectively. YC137 inhibits the binding of the Bid BH3 peptide to Bcl-2, thus disrupting an interaction essential for the antiapoptotic activity of Bcl-2. YC137 selectively induces apoptosis of Bcl-2-dependent cells. YC137 has the potential for breast cancer research .
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-
- HY-P11043
-
|
|
GLP Receptor
Neuropeptide Y Receptor
Arrestin
|
Metabolic Disease
|
|
GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research .
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- HY-14993
-
|
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Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
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- HY-P10415
-
EPI-X4
1 Publications Verification
hSA(408–423) peptide
|
CXCR
|
Infection
Inflammation/Immunology
Cancer
|
|
EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
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-
- HY-14994
-
|
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
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-
- HY-19210
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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-
- HY-116268
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia .
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-
- HY-103363
-
|
|
CCR
Thymidylate Synthase
|
Inflammation/Immunology
Cancer
|
|
SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM. SB-328437 can inhibit eosinophil migration induced by eotaxin, eotaxin-2, and monocyte chemotactic protein-4. In addition, SB-328437 can sensitize 5-FU (HY-90006)-resistant gastric cancer cells. SB-328437 can also reduce the recruitment of neutrophils to the lungs and pulmonary inflammation during acute inflammation. SB-328437 can be used in the research of inflammation-related diseases .
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-
- HY-W044285
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-D-4-Aph(cBm)-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize biologically active peptide mimetics, such as Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph/4Amf(P)-D4Aph/D4Amf(Q)-Leu-ILys-Pro-DAla-NH2 with gonadotropin-releasing hormone (GnRH) antagonist activity .
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-
- HY-107664A
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
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-
- HY-107664
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
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- HY-107664B
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 TFA is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders .
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- HY-150700
-
|
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ERK
|
Metabolic Disease
|
|
RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .
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-
- HY-14993R
-
|
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 (Standard) is the analytical standard of SCH79797. This product is intended for research and analytical applications. SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
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-
- HY-P1656
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
(D-Pro7)-Angiotensin I/II (1-7) is a selective, peptide-based antagonist of Angiotensin-(1-7). (D-Pro7)-Angiotensin I/II (1-7) potently blocks multiple biological effects of Ang-(1-7). (D-Pro7)-Angiotensin I/II (1-7) inhibits the hypertensive response induced by microinjection of Ang-(1-7) into the rostral ventrolateral medulla (RVLM) and abolishes the endothelium-dependent vasorelaxation of mouse. (D-Pro7)-Angiotensin I/II (1-7) can be used for the study of cardiovascular diseases .
|
-
- HY-P10971
-
|
|
CXCR
Apoptosis
VEGFR
GSK-3
Cadherin
Caspase
|
Cancer
|
|
Nef-M1 (Nef-Motif-1) is an antagonist peptide targeting CXCR4 and an apoptosis inducer derived from a myristoylated protein encoded by the nef gene in HIV. Nef-M1 inhibits tumor angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 activates the apoptosis pathway by increasing the level of caspase-3 in cancer cells. Nef-M1 simultaneously inhibits VEGF-A, p-GSK-3β and vimentin, and enhances E-cadherin, thereby inhibiting angiogenesis and EMT processes. Nef-M1 can be used in the study of colorectal cancer and breast cancer .
|
-
- HY-19307
-
|
|
Integrin
Interleukin Related
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
SB-273005 is an orally active non-peptide αvβ3 integrin antagonist with Ki values of 1.2 nM and 0.3 nM for αvβ3 and αvβ5, respectively. SB-273005 blocks the binding of integrins to the RGD sequence in the extracellular matrix. SB-273005 inhibits Rictor phosphorylation and reduces IL-10 secretion. SB-273005 inhibits inflammation, prevents bone loss, regulates vascular smooth muscle function, and reverses pregnancy-induced immune deviation. SB-273005 can be used in the study of rheumatoid arthritis, osteoporosis, and aneurysms. .
|
-
- HY-14994R
-
|
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 (dihydrochloride) (Standard) is the analytical standard of SCH79797 (dihydrochloride). This product is intended for research and analytical applications. SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
|
-
- HY-P1110
-
AF12198
4 Publications Verification
|
Interleukin Related
|
Inflammation/Immunology
|
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo .
|
-
- HY-135446
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
BQ-610 is a selective antagonist of the endothelin A receptor (ETA receptor). BQ-610 specifically blocks the ETA receptor, competitively inhibiting the binding of endothelin-1 (ET-1) (a vasoconstrictive peptide) to the receptor, thereby blocking the effects of ET-1 such as vascular smooth muscle contraction, cell mitosis, and inhibition of hormone secretion. BQ-610 significantly alleviates cerebral vasospasm in rabbits. BQ-610 blocks the bronchial epithelial and pulmonary vascular cell proliferation caused by cigarette smoke in rat models. BQ-610 can delay the natural luteal regression in the cow's uterus. BQ-610 can be used for research on vasospasm, abnormal cell proliferation, and reproductive endocrine disorders .
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-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2276A
-
-
- HY-P0099
-
|
|
nAChR
|
Others
|
|
Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .
|
-
- HY-P5971A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
TCMCB07 TFA, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia .
|
-
- HY-P4874
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity .
|
-
- HY-P5971
-
|
Mifomelatide
|
Melanocortin Receptor
|
Metabolic Disease
|
|
TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia. TCMCB07 has potential transport capabilities .
|
-
- HY-P2268
-
|
|
Amyloid-β
|
Inflammation/Immunology
Cancer
|
|
RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities .
|
-
- HY-P2268A
-
|
|
Amyloid-β
|
Inflammation/Immunology
Cancer
|
|
RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities .
|
-
- HY-P5359
-
-
- HY-P11035
-
|
|
Ephrin Receptor
|
Neurological Disease
Cancer
|
|
APY-d3 is a EphA4-LBD antagonistic peptide with a Kd of 138 nM. APY-d3 is constrained into a bioactive β-hairpin conformation via a head-to-tail disulfide bond. APY-d3 can be used for cancers like gastric and pancreatic cancers and neurodegenerative diseases like amyotrophic lateral sclerosis and Alzheimer’s disease research .
|
-
- HY-P1376
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-P5889
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent .
|
-
- HY-P11214
-
|
H-TL1
|
TNF Receptor
Integrin
NF-κB
ERK
p38 MAPK
JNK
Interleukin Related
|
Inflammation/Immunology
|
|
Hydrostatin-TL1 (H-TL1), a nine-amino-acid peptide, is a TNF-α antagonist. Hydrostatin-TL1 can be isolated from the venom gland of sea snake Hydrophis cyanocinctus. H-TL1 competitively inhibits the interaction between TNF-α/TNFR1 and attenuates the cytotoxicity and inflammation of TNF-α. Hydrostatin-TL1 can be used for TNF-α-associated inflammatory diseases, such as rheumatoid arthritis, osteoporosis and inflammatory bowel disease (IBD) research .
|
-
- HY-P4111
-
|
|
CXCR
|
Cancer
|
|
Peptide R, a cyclic peptide, is a specific CXCR4 antagonist. Peptide R shows outstanding capacities to profoundly remodel the tumor stroma. Peptide R has the potential for tumor research .
|
-
- HY-P10957
-
|
MBX 1416
|
GLP Receptor
|
Metabolic Disease
|
|
Imapextide is a glucagon-like peptide-1 (GLP-1) receptor antagonist that can be used in hypoglycemia research .
|
-
- HY-P10973
-
|
|
CXCR
ERK
|
Cancer
|
|
Peptide R analogue 10 (compound 10) is an analog of the CXCR4 antagonist peptide Peptide R (HY-P4111) with stronger antagonistic potency, specificity and plasma stability. Peptide R analogue 10 can inhibit CXCL12-mediated cell migration, ERK phosphorylation and CXCR4 internalization. Peptide R analogue 10 can be used in the study of CXCR4 overexpressing leukemia and colon cancer .
|
-
- HY-P1376A
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
|
-
- HY-P2612A
-
|
|
TNF Receptor
|
Others
Cancer
|
|
WP9QY, TNF-a Antagonist, TNF-a Antagonist is a biological active peptide. (This cyclic peptide is designed to mimic the most critical tumor necrosis factor (TNF) recognition loop on TNF receptor I. It prevents interactions of TNF with its receptor. This TNF antagonist is a useful template for the development of small molecular inhibitors to prevent both inflammatory bone destruction and systemic bone loss in rheumatoid arthritis.)
|
-
- HY-P2612
-
|
|
TNF Receptor
|
Others
|
|
WP9QY, TNF-a Antagonist, TNF-a Antagonist is a biological active peptide. (This cyclic peptide is designed to mimic the most critical tumor necrosis factor (TNF) recognition loop on TNF receptor I. It prevents interactions of TNF with its receptor. This TNF antagonist is a useful template for the development of small molecular inhibitors to prevent both inflammatory bone destruction and systemic bone loss in rheumatoid arthritis.)
|
-
- HY-16027
-
|
|
GnRH Receptor
|
Endocrinology
|
|
Acyline, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels .
|
-
- HY-P2669
-
-
- HY-P4111A
-
|
|
CXCR
|
Cancer
|
|
Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. Peptide R (TFA) shows outstanding capacities to remodel the tumor stroma. Peptide R (TFA) can be used for solid tumor (glioblastoma, etc.) research .
|
-
- HY-P10938
-
-
- HY-16027A
-
|
|
GnRH Receptor
|
Endocrinology
|
|
Acyline TFA, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels .
|
-
- HY-P5188A
-
-
- HY-P5171
-
|
|
Wnt
|
Cancer
|
|
MDGCEL is a WNT5A peptide, that acts as a WNT5A mimicks and exhibits WNT5A antagonistic activity .
|
-
- HY-P1988
-
-
- HY-P10204
-
|
|
Wnt
|
Cancer
|
|
FZD7 antagonist 1 (peptide 34) is a dFz7-21 analogue. FZD7 antagonist 1 is an FZD7 antagonist that inhibits the wnt3a with IC50 value of 9.2 nM. FZD7 antagonist 1 blocks TcdB−FZD interaction via targeting FZD receptors .
|
-
- HY-P11011
-
|
Pep R54; CXCR4 antagonist peptide 19
|
CXCR
|
Cancer
|
|
Peptide R54 (Pep R54; CXCR4 antagonist peptide 19) is an antagonistic peptide targeting CXCR4 with significant anticancer activity. Peptide R54 inhibits CXCR4-dependent cell migration, epithelial-mesenchymal transition, and lung metastasis development, with better serum stability and higher CXCR4 affinity than the lead compound (IC50=20 nM). Peptide R54 synergizes with anti-PD-1 therapy to exert anti-tumor activity in vivo, enhances granzyme activity, and reduces infiltration of Foxp3 cells. Peptide R54 can be used in the study of colon cancer, ovarian cancer, and melanoma .
|
-
- HY-P1014
-
-
- HY-P1572
-
|
|
Renin
|
Inflammation/Immunology
|
|
Handle region peptide, rat is a prorenin receptor antagonist, suppresses the progression of diabetic nephropathy and has anti-inflammatory in the eye.
|
-
- HY-P4157
-
|
|
MDM-2/p53
Apoptosis
|
Metabolic Disease
|
|
FOXO4-DRI is a cell-permeable peptide antagonist that blocks the interaction of FOXO4 and p53. FOXO4-DRI is a senolytic peptide that induces apoptosis of senescent cells .
|
-
- HY-P4157A
-
|
|
MDM-2/p53
Apoptosis
|
Metabolic Disease
|
|
FOXO4-DRI acetate is a cell-permeable peptide antagonist that blocks the interaction of FOXO4 and p53. FOXO4-DRI acetate is a senolytic peptide that induces apoptosis of senescent cells .
|
-
- HY-135108
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC50 of 4.7 μM .
|
-
- HY-P2319
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-P2319A
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-103473
-
-
- HY-P3557
-
-
- HY-P3227
-
|
XJ735
|
Integrin
|
Inflammation/Immunology
|
|
Cyclo(Ala-Arg-Gly-Asp-Mamb) is a selective RGD peptide antagonist and has the potential for Pulmonary arterial hypertension
Research .
|
-
- HY-P1023
-
|
|
GCGR
|
Metabolic Disease
|
|
VIP(6-28)(human, rat, porcine, bovine) is an effective antagonist of the actions of exogenous vasoactive intestinal peptide (VIP) on cAMP.
|
-
- HY-P10577
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
RAG8 peptide is an antagonist for protease-activated receptor 4 (PAR 4), which inhibits late-stage platelet activation, and reduces thrombosis without altering hemostasis or increasing bleeding risk. RAG8 peptide can be used for atherosclerosis research .
|
-
- HY-P10949
-
|
|
Glycoprotein VI
|
Cardiovascular Disease
|
|
Pep-10L peptide is a glycoprotein VI (GPVI) antagonist with Ki values of 180, 225, and 179 μM for CPR, GPO-1, and Type 1 collagen, respectively. Pep-10L peptide has anti-thrombotic effects .
|
-
- HY-P1271
-
|
Catestatin (cattle)
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-P1119
-
|
|
Formyl Peptide Receptor (FPR)
|
Neurological Disease
|
|
WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide .
|
-
- HY-P3557A
-
-
- HY-P1196
-
-
- HY-P1663
-
|
|
VEGFR
|
Others
|
|
ATWLPPR Peptide is a biological active peptide. (This peptide is a specific VEGFR2/KDR heptapeptide antagonist, it binds VEGFR2 (KDR/flk), completely inhibiting VEGF binding to KDR and preventing VEGF-induced angiogenesis in-vivo. It specifically inhibits human endothelial cell proliferation in-vitro and totally abolishes VEGF-induced angiogenesis in-vivo.)
|
-
- HY-P1119A
-
|
|
Formyl Peptide Receptor (FPR)
|
Neurological Disease
|
|
WRW4 TFA, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 TFA specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide .
|
-
- HY-P10089
-
|
|
Peptides
|
Inflammation/Immunology
|
|
TREM-1 inhibitory peptide M3 is a ligand-dependent TREM-1 antagonist. TREM-1 inhibitory peptide M3 can inhibit systemic and pulmonary pro-inflammatory cytokine and chemokine production and attenuate acute lung injury .
|
-
- HY-W010922
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-Dap(Boc)-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bicyclic peptide tachykinin NK2 antagonists .
|
-
- HY-P3213
-
- HY-P2264
-
|
|
Ephrin Receptor
|
Inflammation/Immunology
|
|
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .
|
- HY-P1271A
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
- HY-P11052
-
|
|
HSP
|
Cancer
|
|
A8 peptide is a Hsp72 antagonist. A8 peptide inhibits tumor progression and metastasis as well as enhances the cancer cells' sensitivity to apoptosis induced by chemotherapeutic agents (such as Cisplatin (HY-17394)) by blocking the Hsp72-TLR2 interaction and the subsequent activation of MDSCs. A8 peptide can be used for cancers research .
|
- HY-P1196A
-
- HY-17446
-
|
HOE 140
|
Bradykinin Receptor
|
Endocrinology
|
|
Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively .
|
- HY-108896
-
|
HOE 140 acetate
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC50 and Ki of 1.07 nM and 0.798 nM respectively .
|
- HY-P5509
-
|
|
Peptides
|
Others
|
|
C5aR1 antagonist peptide is a biological active peptide. (This linear peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions to inhibit C5a binding and function at human and rat C5a receptors. C5a is crucial to triggering cellular immune responses and its overexpression is involved in arthritis, Alzheimer’s disease, cystic fibrosis, systemic lupus erythematosus, and other immunoinflammatory diseases.)
|
- HY-P3212
-
|
|
Neuropeptide Y Receptor
Peptides
|
Cancer
|
|
Allo-aca, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca blocks leptin signaling and action in numerous in vitro and in vivo models .
|
- HY-W013154
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-Tic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as the biotinylated derivative of the opioid receptor antagonist TIPP .
|
- HY-P10278
-
|
|
Peptides
|
Endocrinology
|
|
Anantin binds competitively to the receptor of atrial natriuretic factor (ANF) from bovine adrenal cortex (Kd = 0.6 μM) and acts as natriuretic peptide receptor A antagonist .
|
- HY-P0062
-
- HY-P0062B
-
- HY-P1242
-
- HY-P1454B
-
|
|
Wnt
|
Cancer
|
|
Fz7-21S is a negative control of Fz7-21. Fz7-21 is a potent peptide antagonist of FZD7 receptors .
|
- HY-P0107
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
- HY-P3212A
-
|
|
Neuropeptide Y Receptor
|
Cancer
|
|
Allo-aca TFA, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca TFA blocks leptin signaling and action in numerous in vitro and in vivo models .
|
- HY-P1242A
-
- HY-P1141
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1(9-36)amide is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide acts as an antagonist to the human pancreatic GLP-1 receptor .
|
- HY-P2497
-
|
|
GCGR
|
Neurological Disease
|
|
Exendin (5-39) is a potent glucagon-like peptide 1 (GLP-1) receptor antagonist. Exendin (5-39) improves memory impairment in β-amyloid protein-treated rats .
|
- HY-P11352
-
|
RM26
|
Bombesin Receptor
|
Cancer
|
|
JMV594 (Compound RM 26) is a bombesin analogue with high affinity and antagonistic effect for gastrin releasing peptide receptor (GRPR).JMV594 can be used for the research of cancer, such as Prostate cancer .
|
- HY-P0062A
-
- HY-P1141A
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1(9-36)amide TFA is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide TFA acts as an antagonist to the human pancreatic GLP-1 receptor .
|
- HY-P0264A
-
|
Avexitide acetate
|
GLP Receptor
|
Metabolic Disease
|
|
Exendin(9-39) amide (Avexitide) acetate is a glucagon-like peptide-1 (GLP-1) antagonist that competes with endogenous GLP-1 for the GLP-1R, counteracting the effects of excessive GLP-1 secretion. Exendin(9-39) amide acetate can be utilized in Postbariatric hypoglycemia (PBH) research .
|
- HY-P0264
-
|
Avexitide
|
GLP Receptor
|
Metabolic Disease
|
|
Exendin(9-39) amide (Avexitide) is a glucagon-like peptide-1 (GLP-1) antagonist that competes with endogenous GLP-1 for binding to GLP-1 receptors, thereby antagonizing the effects of excess GLP-1 secretion. Exendin(9-39) amide can be used to study postoperative hypoglycemia (PBH) .
|
- HY-P0107A
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
- HY-P1471
-
|
22-52-Adrenomedullin (human)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
|
- HY-125053A
-
|
|
Glycoprotein VI
|
Cardiovascular Disease
|
|
Batifiban TFA, a cyclic peptide, is an antagonist of platelet glycoprotein GPⅡb/Ⅲa and inhibits platelet aggregation. Batifiban blocks the binding of circulating vitronectin to integrin ανβ3 .
|
- HY-P1277
-
- HY-P1868
-
|
DGEA peptide
|
Integrin
|
Infection
|
|
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors .
|
- HY-P0211
-
|
|
GCGR
|
Cardiovascular Disease
|
|
[Ac-Tyr1,D-Phe2]GRF 1-29, amide (human), a growth hormone releasing factor (GRF) analogue, is a vasoactive intestinal peptide (VIP) antagonist .
|
- HY-P1868A
-
|
DGEA peptide TFA
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors .
|
- HY-P1277A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively .
|
- HY-P4127
-
|
|
Peptides
|
Neurological Disease
|
|
M65 is a deleted peptide of maxadilan (61 a.a.) with deletion of the residues between positions 24 and 42 and is a specific antagonist of PACAP type 1 receptor that inhibits ANP secretion and can be used for relevant researches .
|
- HY-P10474
-
|
|
Drug Isomer
|
Others
|
|
RYTVELA is a deriviative of the peptide antagonist of interleukin-1 receptor 1 (IL-1R1) d-(RYTVELA) (HY-P10353) that contains all L-amino acids .
|
- HY-W041989
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-Oic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as [desArg 10]HOE 140, which has bradykinin B1 antagonist activity .
|
- HY-P4127A
-
- HY-W013153
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-D-Tic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as [desArg 10]HOE 140, which has bradykinin B1 antagonist activity .
|
- HY-P1327
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BVD 10, a neuropeptide Y (NPY) analogue peptide, is a highly selective NPY Y1 receptor antagonist. BVD10 significantly prevents NPY-induced glutamate increase. BVD 10 can be used for seizure research .
|
- HY-P10102
-
Kp7-6
2 Publications Verification
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Kp7-6, a Fas mimetic peptide, is a Fas/FasL antagonist. Kp7-6 protects cells from Fas-mediated apoptosis, and protects mice from Fas-mediated hepatic injury .
|
- HY-P5891
-
|
|
PKC
|
Cardiovascular Disease
|
|
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
|
- HY-W006937
-
|
Boc-p-amino-D-Phe(Fmoc)-OH; Boc-D-phe(4-NH-fmoc)-OH
|
Amino Acid Derivatives
|
Others
|
|
Boc-D-(4-fmoc)-aminophenylalanine (Boc-p-amino-D-Phe(Fmoc)-OH) is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize peptides with gonadotropin-releasing hormone antagonist activity .
|
- HY-P10388
-
|
|
CD47
TGF-β Receptor
|
Cancer
|
|
TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
|
- HY-P5493
-
|
|
Peptides
|
Others
|
|
D-Arg-[Hyp3,Thi5,8,D-Phe7]-Bradykinin is a biological active peptide. (inhibited bradykinin-induced contractions concentration dependently; bradykinin B2 receptor antagonist)
|
- HY-P1285
-
|
Con-R
|
iGluR
|
Neurological Disease
|
|
Conantokin R (Con-R) is an NMDA receptor peptide antagonist with an IC50 of 93 nM. Conantokin R binds Zn 2+ and Mg 2+ with Kds of 0.15 μM and 6.5 μM, respectively. Conantokin R shows anticonvulsant activity .
|
- HY-17446R
-
|
HOE 140 (Standard)
|
Reference Standards
Bradykinin Receptor
|
Endocrinology
|
|
Icatibant (Standard) is the analytical standard of Icatibant. This product is intended for research and analytical applications. Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively .
|
- HY-108896R
-
|
HOE 140 acetate (Standard)
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
Icatibant (acetate) (Standard) is the analytical standard of Icatibant (acetate). This product is intended for research and analytical applications. Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC50 and Ki of 1.07 nM and 0.798 nM respectively .
|
- HY-P1050A
-
|
|
Apolipoprotein
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM .
|
- HY-P6292
-
|
|
PACAP Receptor
|
Neurological Disease
|
|
KS-133 is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 plays an important role in schizophrenia research .
|
- HY-P3117
-
|
Pituitary adenylate cyclase-activating peptide (6-27)
|
Adenylate Cyclase
|
Neurological Disease
|
|
PACAP (6-27) (human, ovine, rat) is a PACAP receptor antagonist that blocks the canine adrenal catecholamine response to exogenous vasoactive intestinal peptide (VIP). PACAP (6-27) (human, ovine, rat) has the potential to study cardiovascular and neurological diseases .
|
- HY-P10465
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain .
|
- HY-P5327
-
|
|
Bcl-2 Family
|
Others
|
|
r8 Bid BH3 is a biological active peptide. (The Bid BH3 is a pro-apoptotic member of the 'BH3-only' subset of BCL-2 family proteins that constitute a critical control point in apoptosis. r8BIDBH3 is lethal to human leukemia cell lines that expresse Bcl-2. The Bcl-2 antagonists may have the potential to be efficacious in cancer therapy. Poly-D-arginine (d-isomer as denoted by rrrrrrrr) is fused to the Bid BH3 peptide to facilitate cellular uptake of the peptide.)
|
- HY-P4776
-
- HY-P1242B
-
|
|
Drug Derivative
|
Inflammation/Immunology
|
|
NEP(1-40), N-terminal uncapped is a NEP(1-40) (HY-P1242) analog without the acetylation modification at the N-terminal. NEP(1-40) is a Nogo-66 receptor (NgR) antagonist peptide .
|
- HY-125053
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Batifiban, a cyclic peptide, is a platelet glycoprotein GPⅡb/Ⅲa antagonist, and inhibits platelet aggregation. Batifiban blocks circulating vitronectin binding to integrin ανβ3, Batifiban can be used for research of acute coronary syndromes .
|
- HY-P10486
-
|
|
Bacterial
|
Infection
|
|
AIP-II is a macrocyclic peptide signaling molecule used for quorum sensing, which can be produced be Staphylococcus aureus. AIP-II binds to AgrC-II receptor, regulates the virulence gene expression in Staphylococcus aureus. AIP-II is an antagonist for AgrC-I receptor .
|
- HY-107080
-
|
|
Integrin
|
Cardiovascular Disease
|
|
RPR-109891 is an orally active glycoprotein IIb/IIIa peptide antagonist. RPR-109891 can decrease platelet count and reduce platelet survival time. RPR-109891 can be used for the research of cardiovascular disease, such as myocardial infarction .
|
- HY-P3542
-
|
|
GCGR
|
Metabolic Disease
|
|
Des His1, Glu8 Exendin-4 is a potent glucagon-like peptide-1 receptor (GLP-1-R) antagonist. Des His1, Glu8 Exendin-4 improves glucose homeostasis by regulating both insulin secretion and glucose production. Des His1, Glu8 Exendin-4 can be used for the research of type 2 diabetic and gastrointestinal .
|
- HY-P1293
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
|
- HY-P6292A
-
|
|
PACAP Receptor
|
Neurological Disease
|
|
KS-133 TFA is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 TFA plays an important role in schizophrenia research .
|
- HY-P10405
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
TAT-D1 peptide is a selective D1-D2 heterogeneous antagonist. TAT-D1 peptide destroys the heterodimer of the D1-D2 receptor by interacting with the specific domain of the D2 receptor through its unique amino acid sequence, in particular the two glutamate residues at the C terminal of the D1 receptor. TAT-D1 peptide can be used to study the role of D1-D2 receptor heterodimers in the regulation of depressive and anxiety-like behaviors .
|
- HY-106268A
-
|
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Larazotide acetate is a peptide which is an orally active zonulin antagonist. Larazotide acetate shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide acetate can be used for the research of celiac disease and infection.
|
- HY-P0097A
-
|
Melanostatine-5 acetate salt
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
- HY-P0097
-
|
Melanostatine-5
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
- HY-P1419
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
AP 811 is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 displays >20000-fold selectivity for NPR3 over NPR1. AP 811 abolishes ANP-induced pump stimulation .
|
- HY-P0102
-
|
|
mAChR
|
Endocrinology
|
|
Dipeptide diaminobutyroyl benzylamide diacetate, a Wagerlin-1-mimicking peptide, is a mAChR antagonist. Dipeptide diaminobutyroyl benzylamide diacetate can induce muscle relaxation. Dipeptide diaminobutyroyl benzylamide diacetate can be used in the research of skin aging, especially facial wrinkles (such as crow's feet and wrinkles around the eyes) .
|
- HY-P10314
-
|
L144-PLP(139-151)
|
Peptides
|
Inflammation/Immunology
|
|
[Leu144]-PLP (139-151) (L144-PLP(139-151)) is a peptide ligand of T cell receptor. [Leu144]-PLP (139-151) is a TCR antagonist for encephalitogenic Th1 clones, blocking their activation .
|
- HY-P1419A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
AP 811 acetate is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 acetate displays >20000-fold selectivity for NPR3 over NPR1. AP 811 acetate abolishes ANP-induced pump stimulation .
|
- HY-P3429
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
- HY-P1143
-
|
|
GCGR
|
Metabolic Disease
|
|
[Des-His1,Glu9]-Glucagon amide is a potent and peptide antagonist of the glucagon receptor, with a pA2 of 7.2. [Des-His1,Glu9]-Glucagon amide is potentially useful in the study of the pathogenesis of diabetes .
|
- HY-P1471A
-
|
22-52-Adrenomedullin (human) (TFA)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
|
- HY-P1293A
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
- HY-106268
-
|
|
Gap Junction Protein
|
Infection
Inflammation/Immunology
|
|
Larazotideis a peptide which is an orally active zonulin antagonist. Larazotide shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide can be used for the research of celiac disease and infection .
|
- HY-P1651
-
SOR-C13
1 Publications Verification
|
TRP Channel
|
Cancer
|
|
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity .
|
- HY-P5645
-
LEAP-2
1 Publications Verification
Human liver expressed antimicrobial peptide-2
|
GHSR
Interleukin Related
IFNAR
TNF Receptor
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
LEAP-2 (Human liver expressed antimicrobial peptide-2) is a GHS-R1a antagonist, with an IC50 of 6.0 nM. LEAP-2 suppresses the orexigenic effect of ghrelin. LEAP-2 attenuates ghrelin-induced growth hormone (GH) release and reduces basal food intake. LEAP-2 exhibits antimicrobial activity against microbial model organisms. LEAP-2 can be used for the study of obesity and infection .
|
- HY-P4072
-
|
|
PD-1/PD-L1
|
Cancer
|
|
(D)-PPA 1 is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy .
|
- HY-P1711
-
|
|
Peptides
|
Cardiovascular Disease
|
|
L 366763 is a potent peptide that acts as a fibrinogen receptor antagonist, preventing collagen-induced platelet aggregation and adhesion. L 366763 inhibits platelet deposition and maintains blood flow in a baboon thrombosis model, significantly prolonging bleeding time. L 366763 has antithrombotic efficacy, whereas recombinant LAPP does not have the same effect .
|
- HY-108055
-
|
|
Urotensin Receptor
Peptides
|
Cardiovascular Disease
|
|
Urantide is a selective and competitive urotensin-II (UT) receptor antagonist peptide (pKB=8.3) that blocks human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide can be used to study the (patho)physiological role of hU-II in the mammalian cardiovascular system .
|
- HY-P1651A
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity .
|
- HY-P1143A
-
|
|
GCGR
|
Metabolic Disease
|
|
[Des-His1,Glu9]-Glucagon amide TFA is a potent and peptide antagonist of the glucagon receptor, with a pA2 of 7.2. [Des-His1,Glu9]-Glucagon amide TFA is potentially useful in the study of the pathogenesis of diabetes .
|
- HY-P4072A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
(D)-PPA 1 TFA is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 TFA serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 TFA binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy .
|
- HY-P3429A
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA TFA is conjugated to the cell permeable peptide TAT47-57. SAMβA TFA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
- HY-P1309
-
- HY-P3343A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells .
|
- HY-P1039
-
|
PHCVPRDLSWLDLEANMCLP
|
Raf
|
Cancer
|
|
R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1 .
|
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
- HY-P2026
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [ 125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells .
|
- HY-P1263
-
- HY-P3226
-
|
|
IGF-1R
|
Metabolic Disease
|
|
JB-1, an IGF-1 peptide analog, is a selective and potent IGF-1R antagonist. JB-1 competes with IGF-1 by binding the IGF-1 receptor. JB-1 prevents the autophosphorylation of IGF-1R, and has no activity in IGF-II .
|
- HY-P1039A
-
|
PHCVPRDLSWLDLEANMCLP TFA
|
Raf
|
Cancer
|
|
R18 TFA is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1 .
|
- HY-P1263A
-
- HY-P7061A
-
|
|
Apelin Receptor (APJ)
CXCR
|
Infection
Endocrinology
|
|
ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
|
- HY-P10135
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
RES-701-1 is a cyclic peptide composed of 16 common L-amino acids, acting as a specific antagonist for the ETB receptor. RES-701-1 can inhibit the binding of 125I-ET-1 (125I-labeled Endothelin (ET)-1) to the ETB receptor, with an IC50 value of 10 nM .
|
- HY-P1795
-
|
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
Boc-dPhe-Leu-dPhe-Leu-Phe (Boc-fLfLF) is a selective N-formyl peptide receptor1 (FPR1) antagonist. Boc-dPhe-Leu-dPhe-Leu-Phe inhibits fMIFL(HY-P0224)-induced NADPH oxidase activity. Boc-dPhe-Leu-dPhe-Leu-Phe can be used for the study of inflammation .
|
- HY-P7061
-
|
|
CXCR
Apelin Receptor (APJ)
|
Infection
Endocrinology
|
|
ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
|
- HY-P1309A
-
|
PAR-4-AP TFA; AY-NH2 TFA
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist .
|
- HY-P10831
-
|
|
VEGFR
|
Cardiovascular Disease
Cancer
|
|
GNQWFI, an anti-Flt1 peptide, is a VEGFR1-specific antagonist. GNQWFI blocks the interaction of VEGFR1 with various VEGFR1 ligands, such as VEGFA, VEGFB, and placental growth factor (PIGF) and inhibits VEGF-induced endothelial cell migration and tube formation. GNQWFI is promising for research of cancer, asthma, and other ocular diseases .
|
- HY-P1159
-
- HY-P1159A
-
|
|
PACAP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
[D-p-Cl-Phe6,Leu17]-VIP TFA is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC50 of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP TFA has no activity on glucagon, secretin or GRF receptors .
|
- HY-P3608
-
|
|
GCGR
|
Metabolic Disease
|
|
[Des-His1,Glu9] Glucagon is a potent glucagon receptor system peptide antagonist. [Des-His1,Glu9] Glucagon enhances the glucose-stimulated release of insulin from pancreatic islet cells. [Des-His1,Glu9] Glucagon can be used to research diabetes .
|
- HY-138106
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-D-Cit-OH is citrulline with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as H-Dmt-D-Cit-Aba-b-Ala-NMe-30,50-(CF3)2-Bn and H-Dmt-D-Cit-Aba-b-Ala-NMe-Bn with neurokinin-1 antagonist activity .
|
- HY-P10896
-
|
|
Bombesin Receptor
|
Cancer
|
|
NOTA-P2-RM26 is an antagonist of Bombesin (HY-P0195) analogs, and the gastrin-releasing peptide receptor (GRPR/BB2) is a molecular target for prostate cancer visualization. NOTA-P2-RM26 is labeled with 111In and 68Ga for prostate cancer imaging studies using PET and SPECT/CT .
|
- HY-P1812
-
AUNP-12
3 Publications Verification
NP-12
|
PD-1/PD-L1
|
Cancer
|
|
AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
- HY-P10373
-
|
|
JAK
IFNAR
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
pJAK2(1001-1013) is a cell-penetrating peptide that corresponds to the activation loop of JAK2 tyrosine kinase and functions as a SOCS1/3antagonist. pJAK2 (1001-1013) blocks SOCS1-mediated negative regulation of immune function, and enhances the biological activity of cytokines such as IFNγ and IL6. pJAK2(1001-1013) inhibits the replication of a broad range of viruses and exerts dose-dependent protective efficacy against lethal viral infections. pJAK2(1001-1013) can be used for the study of immune regulation and infection .
|
- HY-P1812A
-
|
NP-12 TFA
|
PD-1/PD-L1
|
Cancer
|
|
AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
- HY-P10550
-
|
|
VEGFR
|
Cancer
|
|
VGB4 is a VEGF-A and VEGF-B antagonist peptide that duplicates two binding domains of VEGF-B (loop 1 and loop3) and are linked together by the receptor-binding domain of VEGF-A (loop3). VGB4 has significant anti-angiogenic and anti-tumor activities and can regulate tumor growth and metastasis through multiple mechanisms. VGB4 could be used in anti-tumor research .
|
- HY-P1617
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
LY 190388 is a penicillamine-containing enkefa peptide analog with μ receptor agonist activity. LY 190388 showed analgesic effect in inhibiting the writhing response in mice after intracerebroventricular administration. The analgesic effect of LY 190388 is not caused by its δ receptor agonist action, but by its μ receptor agonist activity. When LY 190388 is used together with the δ receptor antagonist ICI 174864, an additive analgesic effect is produced .
|
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
- HY-P2025
-
|
|
Histone Methyltransferase
|
Neurological Disease
|
|
JMV 236 is a cholecystokinin antagonist with appetite-suppressing activity. JMV 236 affects the regulation of food intake through the interaction of the intestinal endogenous peptide PrRP and the CCK1 receptor. The administration of JMV 236 activates PrRP neurons located in the NTS, thereby enhancing its appetite-suppressing effect. JMV 236 has significant effects on areas of the central nervous system associated with food intake, especially during states of starvation .
|
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
- HY-103277A
-
|
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
|
BIM 23042 TFA, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin?B?(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
|
- HY-103277
-
|
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
|
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin?B?(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
|
- HY-P5765
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galanin (1-13)-spantide I is a chimeric peptide composed of the N-terminal fragment of galanin (amino acids 1-13) and spantide, a known substance P receptor antagonist. Galanin (1-13)-spantide I has a high affinity for spinal galanin receptor (Kd=1.16 nM). Galanin (1-13)-spantide I can be used to study the effects of galanin on feeding behavior .
|
- HY-P2380
-
|
TFRGAP
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
PAR3 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 1 (PAR1) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR3 and residues 39-44 of the full-length human sequence. PAR3 (1-6) activates p42/44 MAPK signaling in fibroblasts expressing PAR1, but not PAR3, an effect that can be blocked by the PAR1 antagonist RWJ 56110.
|
- HY-P0262
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM) .
|
- HY-P1454
-
Fz7-21
3 Publications Verification
Ac-LPSDDLEFWCHVMY-NH2
|
Wnt
|
Cancer
|
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs the function of FZD7 in Wnt–β-catenin signalling and stem cell function in intestinal organoids .
|
- HY-P1454A
-
|
Ac-LPSDDLEFWCHVMY-NH2 TFA
|
Wnt
|
Cancer
|
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 TFA impairs the function of FZD7 in Wnt-β-catenin signalling and stem cell function in intestinal organoids .
|
- HY-P0039
-
|
|
Bombesin Receptor
|
Cancer
|
|
BIM-26226 is a selective gastrin-releasing peptide receptor (GRPR) (IC50 = 6 nM) and bombesin receptor (BN receptor) antagonist. BIM-26226 antagonizes BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 is specific for the GRP-preferring BN receptor subtype with no interference with GRP receptor system. BIM-26226 can induce the synthesis of somatostatin receptor but has no significant effect on tumor growth .
|
- HY-P1681
-
|
|
Sodium Channel
|
Neurological Disease
|
|
GpTx-1 is a peptide-based NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 demonstrates potent inhibitory activity against the NaV1.7 channel with an IC50 value of 10 nM, while exhibiting excellent selectivity for NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .
|
- HY-P1681A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
GpTx-1 TFA is a peptide-based NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the NaV1.7 channel with an IC50 value of 10 nM, while exhibiting excellent selectivity for NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .
|
- HY-P11043
-
|
|
GLP Receptor
Neuropeptide Y Receptor
Arrestin
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Metabolic Disease
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GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research .
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- HY-P10415
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EPI-X4
1 Publications Verification
hSA(408–423) peptide
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CXCR
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Infection
Inflammation/Immunology
Cancer
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EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
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- HY-W044285
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Amino Acid Derivatives
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Others
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Fmoc-D-4-Aph(cBm)-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize biologically active peptide mimetics, such as Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph/4Amf(P)-D4Aph/D4Amf(Q)-Leu-ILys-Pro-DAla-NH2 with gonadotropin-releasing hormone (GnRH) antagonist activity .
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- HY-P10456
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Peptides
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Inflammation/Immunology
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[Leu144,Arg147]-PLP (139-151) is a mutant peptide fragment of myelin proteolipid protein (PLP), with the tryptophan and histidine at positions 144 and 147 respectively replaced by leucine and arginine. [Leu144,Arg147]-PLP (139-151) also serves as a T cell receptor (TCR) antagonist for encephalitogenic Th1 clones, blocking their activation in vitro. Furthermore, [Leu144,Arg147]-PLP (139-151) can inhibit the development of experimental autoimmune encephalomyelitis (EAE) .
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- HY-P1656
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Angiotensin Receptor
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Cardiovascular Disease
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(D-Pro7)-Angiotensin I/II (1-7) is a selective, peptide-based antagonist of Angiotensin-(1-7). (D-Pro7)-Angiotensin I/II (1-7) potently blocks multiple biological effects of Ang-(1-7). (D-Pro7)-Angiotensin I/II (1-7) inhibits the hypertensive response induced by microinjection of Ang-(1-7) into the rostral ventrolateral medulla (RVLM) and abolishes the endothelium-dependent vasorelaxation of mouse. (D-Pro7)-Angiotensin I/II (1-7) can be used for the study of cardiovascular diseases .
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- HY-P10971
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CXCR
Apoptosis
VEGFR
GSK-3
Cadherin
Caspase
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Cancer
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Nef-M1 (Nef-Motif-1) is an antagonist peptide targeting CXCR4 and an apoptosis inducer derived from a myristoylated protein encoded by the nef gene in HIV. Nef-M1 inhibits tumor angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 activates the apoptosis pathway by increasing the level of caspase-3 in cancer cells. Nef-M1 simultaneously inhibits VEGF-A, p-GSK-3β and vimentin, and enhances E-cadherin, thereby inhibiting angiogenesis and EMT processes. Nef-M1 can be used in the study of colorectal cancer and breast cancer .
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- HY-P1110
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AF12198
4 Publications Verification
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Interleukin Related
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Inflammation/Immunology
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AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P991415
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AM712
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VEGFR
Tie
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Others
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ASKG-712 (AM712) is a recombinant anti-VEGF humanized monoclonal antibody and Ang-2 antagonist peptide fusion protein. ASKG-712 can be used in Wet age-related macular degeneration and Diabetic macular oedema research .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N2600
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-
-
- HY-N8152
-
-
-
- HY-B0290A
-
-
-
- HY-B0290
-
-
-
- HY-Y0265
-
-
-
- HY-N14982
-
-
-
- HY-N2600R
-
-
-
- HY-P1293
-
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Natural Products
Animals
Source classification
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iGluR
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Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
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-
-
- HY-P1293A
-
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Natural Products
Animals
Source classification
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iGluR
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Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
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-
-
- HY-N2359
-
-
-
- HY-167686
-
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Homopisatin
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Natural Products
Source classification
Plants
Dalbergia variabilis
Fabaceae
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Integrin
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Variabilin (Homopisatin) is a potent RGD-containing antagonist of glycoprotein IIb-IIIa and platelet aggregation inhibitor from the hard tick Dermacentor variabilis. Variabilin potently inhibits platelet aggregation induced by the platelet agonists ADP, collagen, and thrombin receptor peptide SFLLRNP. Variabilin also blocks platelet adhesion to immobilized Fg. In addition, Variabilin inhibits binding of purified human GPIIb-IIIa to immobilized Fg .
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-
-
- HY-B0290AR
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-
-
- HY-B0290R
-
-
-
- HY-Y0265R
-
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Indoline-2,3-dione (Standard)
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Alkaloids
other families
Source classification
Plants
Indole Alkaloids
|
Reference Standards
Monoamine Oxidase
Apoptosis
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Isatin (Standard) is the analytical standard of Isatin. This product is intended for research and analytical applications. Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
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-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-14184S
-
|
|
|
Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .
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-
-
- HY-32709S
-
|
|
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Telcagepant-d8 (MK-0974-d8) is deuterium labeled Telcagepant. Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
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-
-
- HY-W751574
-
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Elagolix-d6 (sodium) (NBI-56418-d6 (sodium)) is deuterium labeled Elagolix sodium. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
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-
-
- HY-10119S
-
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Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
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-
-
- HY-B0290S1
-
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|
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Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
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-
-
- HY-12366S
-
|
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Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-106203A
-
|
SSR-125543 hydrochloride
|
|
Alkynes
|
|
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-106203
-
|
SSR-125543
|
|
Alkynes
|
|
Crinecerfont (SSR-125543) is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-106203B
-
|
(R)-SSR-125543
|
|
Alkynes
|
|
(R)-Crinecerfont is the R-enantiomer of Crinecerfont (HY-106203). Crinecerfont (SSR-125543) is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research. Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
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