GPR Agonists

Cat.No.	Product Name	Information	Product Use Citations
S9477	AH7614	AH7614 (compound 39) is a selective FFA4 (GPR120) antagonist with pIC50s of 7.1 for human FFA4 and 8.1 for mouse FFA4.	Biochem Biophys Res Commun, 2025, 781:152546 Cell Prolif, 2023, e13551. Cell Death Differ, 2021, 10.1038/s41418-021-00887-9
S0135	JMS-17-2	JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. This compound is used in the research of metastatic disease in breast cancer patients.	Int J Oncol, 2022, 60(4)47 Brain Res Bull, 2021, S0361-9230(21)00289-6
S7263	AZD1981	AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2.	Mol Cancer Ther, 2019, 18(11):2097-2110
S0080	SNAP94847 hydrochloride	SNAP 94847 hydrochloride is a high affinity and selective antagonist of the MCH1 receptor with an IC50 of 230 nM for rat MCH1 in FLIPR calcium mobility assay.	J Biol Chem, 2025, 301(5):108486
S6850	NE 52-QQ57	NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. This compound effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with this chemical significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signalling molecules, including tumour necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).	Exp Hematol Oncol, 2024, 13(1):13
E1235	NF-56-EJ40	NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.
S0742	DC260126	DC260126, a small organic antagonist for GPR40 (FFAR1), dose-dependently inhibits GPR40-mediated Ca²⁺ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50=6.28, 5.96, 7.07, 4.58 μM, respectively), reduces GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, suppresses palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells.
E4773^New	NOX-6-18（GPR132-B-160）	NOX-6-18 (GPR132-B-160) is a potent and selective antagonist of GPR132 with an IC50 of 17 nM. It regulates macrophage reprogramming within pancreatic islets, reduces weight gain, and improves glucose metabolism in mice on a high-fat diet.
E0113	GPR84 antagonist 8	GPR84 antagonist 8 is an antagonist of GPR84, which abrogates the enhanced inflammatory response mediated by 6-OAU. It has the potential to reduce the inflammatory responses associated with the activation of the GPR84 receptor.
E0106	ML401	ML401, a potent chemical probe, selectively antagonizes G-protein coupled receptor 183 (GPR183, EBI2) with an IC50 of 1.03 nM, and displays activity in a chemotaxis assay with IC50 of 6.24 nM.
S2822	OC000459	OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2.
S0183	NIBR189	NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.
S6651	G15	G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.	Biol Pharm Bull, 2025, 48(5):657-671 iScience, 2024, 27(3):109125 Nutrients, 2023, 16(1)38
S0851	G-1 (LNS 8801)	G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.	iScience, 2024, 27(3):109125
E0377	CLP-3094	CLP-3094, a potent inhibitor targeting the binding function 3 (BF3) site of androgen receptor (AR), inhibits AR transcriptional activity with IC50 of 4 μM, also is a selective, potent GPR142 antagonist.