Catalog No.
Product Name
Application
Product Information
Citations
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GPR119 agonist
GSK-1292263 is a novel GPR119 agonist.- Inoue A, .et al. , Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
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GPR39 agonist
TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).- Urszula Doboszewska, .et al. , Cell Mol Life Sci, 2023, Apr 25;80(5):133 PMID: 37185787
- Urszula Doboszewska, .et al. , Cells, 2023, Jan 9;12(2):264 PMID: 36672199
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GPR agonist
TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.- Ying Liu, .et al. , Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. , Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. , Sci Rep, 2016, 6: 25912 PMID: 27180622
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GPR40 Inhibitor
GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors. -
GPR4 antagonist
GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM. -
GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. -
GPR40/FFA1 agonist
AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist. -
FFA4/GPR120 agonist
GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively. - Versipelostatin is a novel GRP78/Bip molecular chaperone down-regulator of microbial origin that was isolated from the metabolite of Streptomyces versipellis strain 4083-SVS6.
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GPR139 antagonist
NCRW0005-F05, first antagonist selective for GPR139 (IC50 value 0.21 uM); a useful tool to study GPR139 pharmacology, especially in combination with the GPR139 agonist JNJ 63533054. -
GPR35/CXCR8 agonist
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8. -
GPR55 antagonist
CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. -
FAA1 agonist
FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54. -
EBI2 inverse agonist
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM. -
GPR40 agonist
Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. -
FFAR1/GPR40 activator
GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes. -
GPR120 agonist
GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate. -
brain-penetrant GPR88 agonist
RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. -
GPR35/CXCR8 agonist
Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8. -
GPR40/FFAR1 agonist
GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1). -
Gpr120 agonist
GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of ?7.62. -
hGPR91 antagonist
HGPR91 antagonist 1 is a potent and selective small molecule hGPR91 antagonist with an IC50 of 7 μM. -
GPR40 full agonist
GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively. -
GPR4 antagonist
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. Anti-inflammatory activities. -
GPR120 agonist
GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
