Search Result
Results for "
B1 antagonist
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-19900
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- HY-15039
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Bradykinin Receptor
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Metabolic Disease
Inflammation/Immunology
Endocrinology
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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.
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- HY-15043
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Bradykinin Receptor
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Inflammation/Immunology
Endocrinology
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ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
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- HY-P5518A
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- HY-P4676
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- HY-158262
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Bradykinin Receptor
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Neurological Disease
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Bradykinin B1 receptor antagonist 1 (compound 6B) is a potent and cross the blood-brain barrier bradykinin B1 antagonist. Bradykinin B1 receptor antagonist 1 has the potential for the research of pain .
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- HY-P2109
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Bradykinin Receptor
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Inflammation/Immunology
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JMV-1645 is a potent and selective B1 bradykinin receptor antagonist with a Ki value of 0.023 nM on the human cloned B1 receptor. JMV-1645 can be utilized in trauma and infection research .
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- HY-P3232
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- HY-103294
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Endogenous Metabolite
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Others
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R892 is a selective and efficient bradyKinin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability .
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- HY-P5518
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- HY-103290
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Bradykinin Receptor
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Others
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R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
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- HY-W041989
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Amino Acid Derivatives
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Others
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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 .
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- HY-W013153
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Amino Acid Derivatives
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Others
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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 .
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- HY-100301
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Bradykinin Receptor
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Inflammation/Immunology
Endocrinology
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FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC50 value of 65 nM and no binding affinity for the B1 receptor.
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- HY-10799
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Complement System
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Cancer
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EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2 .
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- HY-100827
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LF22-0542
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Bradykinin Receptor
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Inflammation/Immunology
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Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model .
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- HY-168906
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Bradykinin Receptor
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Neurological Disease
Inflammation/Immunology
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BI-113823 is an orally active and selective bradykinin B1 receptor antagonist. BI-113823 can reduce complete Freund's adjuvant (HY-153808)-induced mechanical hyperalgesia in rats. BI-113823 can be used for the research of chronic inflammatory pain .
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- HY-15041
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Bradykinin Receptor
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Inflammation/Immunology
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NVP-SAA164 is an orally active nonpeptide kinin B1 receptor antagonist. NVP-SAA164 reverses CFA (Complete Freund's adjuvant) (HY-153808)-induced mechanical hyperalgesia and desArg10KD-induced hyperalgesia in hB1-KI mice, and is inactive in a model of inflammatory pain in wild-type mice .
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- HY-17617
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Z-360
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Cholecystokinin Receptor
Ephrin Receptor
Interleukin Related
VEGFR
HIF/HIF Prolyl-Hydroxylase
Akt
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Neurological Disease
Cancer
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Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
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- HY-101343
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5-HT Receptor
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Neurological Disease
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RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
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- HY-15042
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Bradykinin Receptor
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Metabolic Disease
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MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .
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- HY-14575
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Z-360 hemicalcium
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Cholecystokinin Receptor
Ephrin Receptor
Interleukin Related
VEGFR
HIF/HIF Prolyl-Hydroxylase
Akt
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Neurological Disease
Cancer
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Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain .
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- HY-17617R
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Cholecystokinin Receptor
Ephrin Receptor
Interleukin Related
VEGFR
HIF/HIF Prolyl-Hydroxylase
Akt
|
Neurological Disease
Cancer
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Nastorazepide (Standard) is the analytical standard of Nastorazepide. This product is intended for research and analytical applications. Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
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- HY-W008038
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iGluR
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Others
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NMDAR antagonist 3 (Compound 2) is an antagonist of the NMDA receptor. NMDAR antagonist 3 has a certain but weak inhibitory activity against the NR1A/2B subtype of the NMDA receptor .
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- HY-155061
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Cytochrome P450
Aryl Hydrocarbon Receptor
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Cancer
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hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC50=3.6 nM),as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells .
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- HY-101356
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mGluR
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Neurological Disease
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CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of metabotropic glutamate receptor 1b (mGluR1b) .
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-
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- HY-114097A
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CCR
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Inflammation/Immunology
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CCR1 antagonist 11 hydrochloride (A1B1) is an orally active CCR1 antagonist with the IC50 values of 0.03 μM, 0.58 μM and 0.32 μM for hCCR1, mCCR1 and rCCR1, respectively. CCR1 antagonist 11 hydrochloride can be used in the study of rheumatoid arthritis and other related inflammatory diseases .
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- HY-126123
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iGluR
Potassium Channel
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Neurological Disease
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NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier .
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- HY-114246
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Androgen Receptor
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Cancer
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ONC1-13B is a potent androgen receptor (AR) antagonist with the activity of effectively inhibiting PSA expression in prostate cancer cells. ONC1-13B can effectively inhibit PSA expression and prostate cancer cell proliferation under DHT stimulation. ONC1-13B exerts its anti-tumor effect by preventing androgen from binding to AR and its nuclear translocation .
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- HY-14348
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
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GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities .
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- HY-P3209
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- HY-121392
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases .
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- HY-169187
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Bacterial
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Cancer
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Antibacterial agent 247 (compund 30b) is a bacterial antagonist that significantly inhibits the formation of Pseudomonas aeruginosa biofilm (IC50=5.8 μM) and multiple virulence phenotypes, and enhances its interaction with Tob Antibacterial activity of combined therapy with ampicillin and polymyxin B .
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- HY-101043
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Sigma Receptor
iGluR
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Neurological Disease
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4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection .
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- HY-107707
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iGluR
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Neurological Disease
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TCS 46b (Compound 46b) is a potent, selective and orally active NMDA NR1A/2B receptor antagonist with an IC50 of 5.3 nM . TCS 46b 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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- HY-100794
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5-HT Receptor
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Neurological Disease
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GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research .
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- HY-123869
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5-HT Receptor
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Neurological Disease
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GR127935 is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 can be used in neurological disease research .
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- HY-N6771
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Calcium Channel
5-HT Receptor
MDM-2/p53
Apoptosis
RSV
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Infection
|
Cyclopiazonic acid is an endoplasmic reticulum calcium ATPase (ECAs) inhibitor and human respiratory syncytial virus (RSV) inhibitor (EC50 value of 4.13 μ M), which can reduce the antagonistic effect of 5-HT receptors in rat thoracic aorta, induce p53 dependent cell apoptosis and reproductive toxicity in mouse testes, and inhibit the biological activation of aflatoxin B [1][4][5].
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- HY-172884
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Cholinesterase (ChE)
iGluR
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Neurological Disease
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MDAR IN-1 (Compound 5m) is a brain-penetrant inhibitor of acetylcholinesterase (AChE) and antagonist of the GluN1/GluN2B subtype of NMDAR receptor. MDAR IN-1 effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR, reducing excitatory neurotoxicity. MDAR IN-1 is promising for research of Alzheimer's disease .
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- HY-13457
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TCN 201
1 Publications Verification
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iGluR
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Neurological Disease
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TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDA receptor, with a pIC50 of 6.8. TCN 201 is selective for GluN1/GluN2A NMDA receptor over GluN1/GluN2B NMDA receptor (pIC50<4.3) .
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- HY-107018
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AR-A 000002
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5-HT Receptor
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Neurological Disease
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AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
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- HY-155735
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iGluR
Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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AChE/Aβ-IN-2 (compound 33) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC50 of 135 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 5.054 μM. AChE/Aβ-IN-2 also inhibits Aβ aggregation and shows good blood-brain barrier permeability. AChE/Aβ-IN-2 improves cognitive and spatial memory impairment in rats model .
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- HY-155733
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iGluR
Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
|
AChE/Aβ-IN-1 (compound 32) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with an IC50 of 86 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 3.876 μM. AChE/Aβ-IN-1 also inhibits Aβ aggregation and shows good blood-brain barrier permeability and neuroprotection. AChE/Aβ-IN-1 improves cognitive and spatial memory impairment in rats model .
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- HY-12882
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Ifenprodil
Maximum Cited Publications
7 Publications Verification
NP-120; RC-61-91
|
iGluR
Adrenergic Receptor
Potassium Channel
Calcium Channel
Influenza Virus
|
Infection
Neurological Disease
|
Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
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- HY-172213
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iGluR
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Neurological Disease
|
(3S,6R)-NML is a NMDA receptor antagonist, with pIC50s of 4.8 (GluN1-GluN2A), 4.6 (GluN1-GluN2B), 5.0 (GluN1-GluN2C), 5.0 (GluN1-GluN2D) respectively. (3S,6R)-NML can be used for depression research .
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- HY-12882A
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NP-120 tartrate; RC-61-91 tartrate
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iGluR
Adrenergic Receptor
Potassium Channel
Calcium Channel
Influenza Virus
|
Infection
Neurological Disease
|
Ifenprodil (NP-120) tartrate, a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate is an α1 adrenergic receptor antagonist. Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil tartrate has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil tartrate can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
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- HY-B0822S1
-
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GABA Receptor
Cytochrome P450
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Inflammation/Immunology
|
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
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-
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- HY-12882AR
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NP-120 tartrate (Standard); RC-61-91 tartrate (Standard)
|
iGluR
Potassium Channel
|
Neurological Disease
|
Ifenprodil (tartrate) (Standard) is the analytical standard of Ifenprodil (tartrate). This product is intended for research and analytical applications. Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator .
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- HY-12962A
-
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iGluR
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Neurological Disease
|
NMDA-IN-1 dihydrochloride is a selective NMDA NR2B antagonist with a Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM. NMDA-IN-1 dihydrochloride inhibits Glu/Gly stimulated Ca2+ flux in Ltk- cells expressing the hNR1a/NR2B with a IC50 of 9.7 nM. NMDA-IN-1 dihydrochloride has no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor. NMDA-IN-1 dihydrochloride shows excellent activity in the mechanical hyperalgesia assay in rats. NMDA-IN-1 dihydrochloride can be used for the study of stroke, Parkinson, and neuropathic pain .
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-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5518A
-
-
- HY-P4676
-
-
- HY-103290
-
|
Bradykinin Receptor
|
Others
|
R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
|
-
- 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-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-P2109
-
|
Bradykinin Receptor
|
Inflammation/Immunology
|
JMV-1645 is a potent and selective B1 bradykinin receptor antagonist with a Ki value of 0.023 nM on the human cloned B1 receptor. JMV-1645 can be utilized in trauma and infection research .
|
-
- HY-P3232
-
-
- HY-103294
-
|
Endogenous Metabolite
|
Others
|
R892 is a selective and efficient bradyKinin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability .
|
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- HY-P5518
-
-
- HY-P3209
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N6771
-
-
-
- HY-12882A
-
-
-
- HY-12882AR
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NP-120 tartrate (Standard); RC-61-91 tartrate (Standard)
|
Alkaloids
Piperidine Alkaloids
Crassulaceae
Source classification
Sedum sarmentosum Bunge
Plants
|
iGluR
Potassium Channel
|
Ifenprodil (tartrate) (Standard) is the analytical standard of Ifenprodil (tartrate). This product is intended for research and analytical applications. Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0822S1
-
|
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
|
-
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