Search Result
Results for "
agonist potency
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101039A
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Opioid Receptor
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Neurological Disease
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AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
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- HY-107539
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GPR35
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Others
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GPR35 agonist 4 (compound 10) is a potent GPR35 agonist with an pEC50 of 5.86. GPR35 agonist 4 shows high potency human and rat GPR35. Mutation of arginine 3.36 eliminates agonist function of GPR35 agonist 4 .
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- HY-147637
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Ephrin Receptor
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Cancer
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EphA2 agonist 1 (Compound 7bg) is a potent EphA2 receptor agonist. EphA2 agonist 1 shows great potency and selectivity toward EphA2 overexpressed glioblastoma cells and stimulates EphA2 phosphorylation .
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- HY-117918
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- HY-148524
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mAChR
Adrenergic Receptor
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Cardiovascular Disease
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β2AR/M-receptor agonist-1 (example 131) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-1 shows potency to β2 adrenoceptor with an EC50 value of 9.2 nM. β2AR/M-receptor agonist-1 also has potency to muscarinic receptor with a Ki value of 30.2 nM. β2AR/M-receptor agonist-1 shows MABA potency with an EC50 value of 4.0 nM .
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- HY-101039
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- HY-123428
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- HY-146438
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PPAR
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Cancer
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PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
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- HY-146439
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PPAR
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Cancer
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PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
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- HY-161105
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5-HT Receptor
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Others
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FPIP is a selectivity agonist of 5-HT1A with a functional potency (pEC50=8.92) .
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- HY-148525
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β2AR/M-receptor agonist-2
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mAChR
Adrenergic Receptor
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Cardiovascular Disease
Inflammation/Immunology
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β2AR/M-receptor agonist-2 (compound 15) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-2 shows potency to β2 adrenoceptor with an EC50 value of 3.7 nM. β2AR/M-receptor agonist-2 also has potency to human cloned M3 receptor with a Ki value of 0.73 nM. β2AR/M-receptor agonist-2 is a potent bronchodilator, it can be used for the research of chronic obstructive pulmonary disease (COPD) .
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- HY-W270810
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Nuclear Hormone Receptor 4A/NR4A
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Cancer
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NR4A agonist-1, a fatty acid mimetic (FAM), is a potent NR4A agonist. NR4A agonist-1 exhibits high agonist potency on NR4A receptors Nurr1, Nur77, and NOR-1, with EC50s of 0.09 μM, 0.04 μM, and 0.15 μM, respectively .
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- HY-108258
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GPR119
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Endocrinology
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PSN 375963 is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 shows similar potency to the endogenous agonist oleoylethanolamide (OEA) .
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- HY-108258A
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GPR119
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Endocrinology
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PSN 375963 hydrochloride is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 hydrochloride shows similar potency to the endogenous agonist oleoylethanolamide (OEA) .
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- HY-15436
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iGluR
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Neurological Disease
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L-687414 is an orally active glycine-site NMDA receptor antagonist or low-potency partial agonist. L-687414 has anticonvulsant activity .
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- HY-14297
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Adrenergic Receptor
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Endocrinology
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Milveterol is a long-acting β(2)-adrenoceptor agonist with high binding activity. Milveterol exhibits high potency in vitro and a prolonged duration of action in a guinea pig bronchoprotection model. Milveterol has been structurally optimized to show enhanced binding potency compared to its parent monomer .
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- HY-110238
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MK6-83
1 Publications Verification
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TRP Channel
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Metabolic Disease
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MK6-83 is a new candidate agonist of TRPML1 with an improved efficacy and potency. MK6-83 has the potential for Mucolipidosis type IV study .
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- HY-133036
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Apelin Receptor (APJ)
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Cardiovascular Disease
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APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure .
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- HY-145362
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LPL Receptor
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Others
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S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).
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- HY-P2249
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Arrestin
Apelin Receptor (APJ)
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Cardiovascular Disease
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ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .
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- HY-121885
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LMD-009
2 Publications Verification
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CCR
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Metabolic Disease
Endocrinology
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LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM .
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- HY-112185
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LY3502970; GLP-1 receptor agonist 1
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GCGR
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Metabolic Disease
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Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete .
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- HY-P10673
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GHSR
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Metabolic Disease
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KwFwLL-NH2, a hexapeptide, is a ghrelin receptor ligand. KwFwLL-NH2 can act as a specific inverse agonist at the ghrelin receptor but with moderate potency (EC50=45.6 nM) .
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- HY-P11246
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RXFP Receptor
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Metabolic Disease
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A13:B7-24-GG is an engineered analogue of insulin-like peptide 5 (INSL5), a selective RXFP4 agonist with a Ki value of 2.29 nM. A13:B7-24-GG has an extremely low binding affinity for RXFP3 (Ki = 602.56 nM) and an inhibitory effect on cAMP (EC50) of 1.17 nM. Activation of RXFP4 by A13:B7-24-GG leads to the recruitment of β-Arrestin2, with an EC50 of 22.39 nM. A13:B7-24-GG can be used for research on chronic constipation .
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- HY-119775
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Others
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Others
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U92016A is a potent and selective agonist of the 5-HT1A receptor, with activities such as high affinity binding to the 5-HT1A receptor in vitro, causing a decrease in body temperature in vivo, and high potency and high intrinsic activity as an agonist in single-cell firing studies.
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- HY-112185A
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LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate
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GCGR
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Metabolic Disease
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Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete .
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- HY-131961
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VD/VDR
HDAC
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Cancer
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Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities .
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- HY-107327
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(±)-Carazolol; DL-Carazolol; Suacron
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Adrenergic Receptor
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Cardiovascular Disease
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Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
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- HY-161107
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GPR84
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Inflammation/Immunology
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OX04529 (compound 69) is a potent, selective and orally active agonist of GPR84. OX04529 inhibits FSK-induced cAMP production with an EC50 of 0.0185 nM. OX04529 displayed excellent potency, high G-protein signaling bias .
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- HY-118190
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Prostaglandin Receptor
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Endocrinology
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AL 8810 methyl ester is a prostaglandin F(2α) analog and a prostaglandin F(2α) receptor agonist. Can competitively antagonize the effects of the FP receptor agonist Fluprostenol (HY-108560). AL 8810 methyl ester has no significant potency against TP, DP, EP(2), EP(4) receptor subtypes in cell lines .
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- HY-129683
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PPAR
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Metabolic Disease
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AM3102 is an oleoylethanolamide (OEA) analog. AM3102 is an endogenous high-affinity PPAR-alpha agonist. AM3102 resists enzymatic hydrolysis, activates PPAR-alpha with high potency in vitro, and persistently reduces feeding when administered in vivo either parenterally or orally .
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- HY-100677
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CXCR
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Endocrinology
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VUF11207 (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7 .
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- HY-175486
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Opioid Receptor
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Neurological Disease
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KOR agonist 6 is a KOR agonist (Ki = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [ 35S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects .
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- HY-W040221
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Platelet-activating Factor Receptor (PAFR)
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Metabolic Disease
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Butanoyl PAF, a compound closely related to Azelaoyl PC (HY-134154), maintains over 10% of the agonist potency of platelet-activating factor (PAF). Butanoyl PAF's concentration in oxidized low-density lipoprotein surpasses that of enzymatically generated PAF by more than 100-fold .
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- HY-128865
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Opioid Receptor
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Neurological Disease
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BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects .
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- HY-14229R
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G protein-coupled Bile Acid Receptor 1
Calcium Channel
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Metabolic Disease
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TGR5 Receptor Agonist (Standard) is the analytical standard of TGR5 Receptor Agonist. This product is intended for research and analytical applications. TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
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- HY-14229
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CCDC
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G protein-coupled Bile Acid Receptor 1
Calcium Channel
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Metabolic Disease
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TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca 2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
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- HY-147707
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Cannabinoid Receptor
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Others
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Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
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- HY-126351
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- HY-107327R
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(±)-Carazolol (Standard); DL-Carazolol (Standard); Suacron (Standard)
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Reference Standards
Adrenergic Receptor
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Cardiovascular Disease
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Carazolol (Standard) is the analytical standard of Carazolol. This product is intended for research and analytical applications. Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
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- HY-B1658
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(R)-Frovatriptan; SB 209509; VML 251
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5-HT Receptor
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Neurological Disease
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Frovatriptan is a potent 5-HT1B//D receptor agonist and has the highest 5-HT1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura .
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- HY-P11320
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Amylin Receptor
CGRP Receptor
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Metabolic Disease
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Davalintide is an Amylin (HY-P1464)-mimetic peptide with greater potency and longer-lasting effects. Davalintide is a potent agonist of amylin receptor (IC50 = 0.04 nM), calcitonin receptor (IC50 = 0.06 nM) and calcitonin related peptide receptor (CGRP receptor) (IC50 = 3.1 nM). Davalintide shows stronger potency to Amylin to activate cyclic AMP production through the calcitonin receptor (EC50 = 1.4 nM). Davalintide regulates blood sugar and weight through various mechanisms such as delaying gastric emptying, inhibiting glucagon secretion, and reducing food intake. Davalintide can be used for the studies of anti-obesity and anti-diabetes .
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- HY-10624
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THIQ
1 Publications Verification
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Melanocortin Receptor
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Metabolic Disease
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THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .
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- HY-109009
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UCB-0942
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GABA Receptor
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Neurological Disease
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Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
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- HY-10569
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ACT-128800
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LPL Receptor
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Inflammation/Immunology
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Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-123459
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ABT-232; NS-49; PNO-49B
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Adrenergic Receptor
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Endocrinology
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Garomefrine hydrochlorid (ABT-232) is an α1A-adrenergic agonist with the potential to inhibit urinary incontinence. Garomefrine hydrochlorid showed the greatest contractility in pig nasal mucosal vessels. The biological activity of Garomefrine hydrochlorid has been shown to give it a competitive advantage compared to other drugs. The potency of Garomefrine hydrochlorid makes it a valuable research object in related research .
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- HY-B1658S
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(R)-Frovatriptan-d3 hydrochloride; SB 209509-d3 hydrochloride; VML 251-d3 hydrochloride
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5-HT Receptor
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Neurological Disease
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Frovatriptan-d3 (hydrochloride) is the deuterium labeled Frovatriptan . Frovatriptan is a potent 5-HT1B//D receptor agonist and has the highest 5-HT1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura .
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- HY-16673
-
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GPR119
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Metabolic Disease
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PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders .
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- HY-124209
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Prostaglandin Receptor
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Endocrinology
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9-keto Fluprostenol is an analog of prostaglandin E2 (PGE2) with structural modifications intended to give it a prolonged half-life and greater potency. Fluprostenol is a well-studied, potent analog of PGF2α and acts primarily through the FP receptor. Oxidation at C-9 of fluprostenol yields 9-keto fluprostenol. It is anticipated that this analog will have strong affinity for EP receptors and act as a PGE2 agonist.
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- HY-P10716
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GLP Receptor
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Metabolic Disease
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Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in G protein-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .
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- HY-126252
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ROR
Interleukin Related
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Inflammation/Immunology
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A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation .
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- HY-125996
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FXR
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Inflammation/Immunology
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NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease .
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- HY-10569R
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ACT-128800 (Standard)
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Reference Standards
LPL Receptor
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Inflammation/Immunology
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Ponesimod (Standard) is the analytical standard of Ponesimod. This product is intended for research and analytical applications. Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-116149
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nAChR
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Others
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A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
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- HY-P5894
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Galanin-like peptide (3-32)
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Neuropeptide Y Receptor
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Neurological Disease
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human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with high affinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
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- HY-109009A
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(S)-UCB-0942
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GABA Receptor
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Neurological Disease
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(S)-Padsevonil is the S-enantiomer of Padsevonil (HY-109009).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
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- HY-106481
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GPR35
Histamine Receptor
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Inflammation/Immunology
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Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide .
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- HY-106963
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LGD1550
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RAR/RXR
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Cancer
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ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
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- HY-114678
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5-HT Receptor
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Neurological Disease
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LY302148 is a receptor ligand for 5-HT1F. Compared to the Emax of 5-HT, LY302148 behaves as a partial agonist for the 5-HT1F receptor. In the [ 35S]GTPγS binding assay targeting human 5-HT1F receptors, LY302148 exhibits good potency with an EC50 value of 5.23 nM. LY302148 can be used in the research of migraine .
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- HY-116679
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17-Trifluoromethylphenyl trinor PGF2α
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Prostaglandin Receptor
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Endocrinology
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A number of 17-phenyl trinor prostaglandin F2α (17-phenyl trinor PGF2α) derivatives have been approved for glaucoma. Of these, the unsubstituted or meta-substituted aromatic derivatives are the most potent FP receptor agonists.4 17-trifluoromethylphenyl trinor PGF2α bears an aromatic ring which is reminiscent of the trifluoromethyl-phenoxy ring of travoprost ((+)-fluprostenol isopropyl ester). As an ocular hypotensive agent, it would be expected that 17-trifluoromethylphenyl trinor PGF2α would act very much like the free acid of travoprost. 17-phenyl trinor PGF2α is a potent luteolytic, with a potency equal to or greater than fluprostenol and cloprostenol.
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- HY-124283
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Endogenous Metabolite
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Inflammation/Immunology
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LEI-101 free base is a selective and orally bioavailable CB2 receptor agonist with the potential to inhibit diseases associated with inflammation and/or oxidative stress. LEI-101 free base has a binding potency to CB2 receptors that is approximately 100 times higher than that to CB1 receptors. Its pEC50 value on CB2 receptors is 8, while its pKi value on hERG is less than 4. LEI-101 may have an inhibitory effect on conditions such as kidney disease .
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- HY-10569S
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ACT-128800-d4
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Isotope-Labeled Compounds
LPL Receptor
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Others
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Ponesimod-d4 (ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-121787
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OLC20
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Olfactory Receptor
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Others
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OX1a (OLC20) is an Orco antagonist with non-competitive activity that inhibits the activation of oxygen odor receptors (ORs). OX1a is able to reduce the activation of ORs by competitively inhibiting the effects of Orco agonists. OX1a also shows non-competitive inhibition of odor molecules, which may affect the olfactory-mediated behavior of insects. Through structural optimization, OX1a analogs have shown higher antagonistic potency, indicating that this type of compound may have application potential in a wide range of insect species .
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- HY-10569S1
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ACT-128800-d7
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Isotope-Labeled Compounds
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Others
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Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
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- HY-130311
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2-Monolinolein; 2-Monolinoleoylglycerol
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Cannabinoid Receptor
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Neurological Disease
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2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
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- HY-137055
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Others
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Others
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PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
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- HY-155811
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iGluR
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Neurological Disease
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DQP-997-74 (compound 2i) is a selective negative allosteric modulator of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC50: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases .
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- HY-103120
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5-HT Receptor
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Neurological Disease
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Org37684 is a highly potent 5-HT2C receptor agonist (pEC50=8.17). Org37684 exhibits a rank order of potency of 5-HT2C>5-HT2B>5-HT2A. Its selectivity for the 5-HT2C receptor is approximately 2.5 times over the 5-HT2B (pEC50=7.96) and ten times for the 5-HT2A (pEC50=7.11) receptor .
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- HY-131615
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Sodium Channel
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Others
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TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na 2+ mobilisation from TPC2 than TPC-A1-N (HY-131614). TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells .
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- HY-W770198
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2-Monolinolein-d5; 2-Monolinoleoylglycerol-d5
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Isotope-Labeled Compounds
Cannabinoid Receptor
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Neurological Disease
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2-Linoleoyl glycerol-d5 (2-Monolinolein-d5; 2-Monolinoleoylglycerol-d5) is the deuterium labeled 2-Linoleoyl glycerol (HY-130311). 2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
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- HY-171807
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nAChR
STAT
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Neurological Disease
Inflammation/Immunology
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TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2249
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Arrestin
Apelin Receptor (APJ)
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Cardiovascular Disease
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ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .
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- HY-P10716
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GLP Receptor
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Metabolic Disease
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Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in G protein-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .
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- HY-P10673
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GHSR
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Metabolic Disease
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KwFwLL-NH2, a hexapeptide, is a ghrelin receptor ligand. KwFwLL-NH2 can act as a specific inverse agonist at the ghrelin receptor but with moderate potency (EC50=45.6 nM) .
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- HY-P11246
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RXFP Receptor
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Metabolic Disease
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A13:B7-24-GG is an engineered analogue of insulin-like peptide 5 (INSL5), a selective RXFP4 agonist with a Ki value of 2.29 nM. A13:B7-24-GG has an extremely low binding affinity for RXFP3 (Ki = 602.56 nM) and an inhibitory effect on cAMP (EC50) of 1.17 nM. Activation of RXFP4 by A13:B7-24-GG leads to the recruitment of β-Arrestin2, with an EC50 of 22.39 nM. A13:B7-24-GG can be used for research on chronic constipation .
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- HY-P11320
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Amylin Receptor
CGRP Receptor
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Metabolic Disease
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Davalintide is an Amylin (HY-P1464)-mimetic peptide with greater potency and longer-lasting effects. Davalintide is a potent agonist of amylin receptor (IC50 = 0.04 nM), calcitonin receptor (IC50 = 0.06 nM) and calcitonin related peptide receptor (CGRP receptor) (IC50 = 3.1 nM). Davalintide shows stronger potency to Amylin to activate cyclic AMP production through the calcitonin receptor (EC50 = 1.4 nM). Davalintide regulates blood sugar and weight through various mechanisms such as delaying gastric emptying, inhibiting glucagon secretion, and reducing food intake. Davalintide can be used for the studies of anti-obesity and anti-diabetes .
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- HY-P5894
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Galanin-like peptide (3-32)
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Neuropeptide Y Receptor
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Neurological Disease
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human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with high affinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-10569S1
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Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
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- HY-B1658S
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Frovatriptan-d3 (hydrochloride) is the deuterium labeled Frovatriptan . Frovatriptan is a potent 5-HT1B//D receptor agonist and has the highest 5-HT1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura .
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- HY-10569S
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Ponesimod-d4 (ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-W770198
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2-Linoleoyl glycerol-d5 (2-Monolinolein-d5; 2-Monolinoleoylglycerol-d5) is the deuterium labeled 2-Linoleoyl glycerol (HY-130311). 2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
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