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GPR G protein-coupled receptor


Cat.No.  Name Information
M22486 AH-7614 AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6).
M21826 AM-1638 AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
M20180 WAY-388798 WAY-388798 is a agonist of free fatty acid receptor 1 (GPR40)
M10634 NE 52-QQ57 NE 52-QQ57 is an orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 significantly inhibited the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor 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).
M10562 GPR81 agonist 1 GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50 values of 58 nM and 50 nM for human and mouse GPR81, respectively.
M10469 MCH TFA (human, mouse, rat) MCH TFA (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively.
M9494 AF64394 AF64394 is a selective GPR3 inverse agonist with a pIC50 of 7.3.
M9245 GTPL5846 GTPL5846 (6-OAU) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
M8948 TUG-891 TUG-891, a selective agonist of FFAR4/GPR120, promoted the intracellular triglyceride accumulation in a dose-dependent manner.
M8822 TUG-424 TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM.
M7541 TUG-770 Tug-770 is a potent, selective, orally active GPR40/FFA1 agonist with an EC50 of 6 nM against human FFA1. Tug-770 has higher selectivity to FFA1 than FFA2, FFA3, FFA4, PPARγ, other receptors, transporters and enzymes.
M6454 AR420626 AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, GPR41) with IC50 of 117 nM.
M6257 ONC212 ONC212, a fluorinated-ONC201 analogue, is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.
M6141 NIBR189 NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional).
M5729 Latanoprost Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
M5292 GPR120-IN-1 GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of 7.62.
M5187 GSK137647A GSK137647A is a selective FFAR4 (GRP120) agonist for human, Mouse and Rat FFA4 with pEC50 values of 6.3, 6.2 and 6.1, respectively. GSK137647A induces insulin secretion and inhibits epithelial ion transport.
M3773 PSN-375963 PSN 375963 is an effective GPR119 agonist with EC50 of 8.4 and 7.9 μM for human and mice, respectively. PSN 375963 showed similar potency to endogenous oleoylethanolamide (OEA).
M3771 PSN632408 PSN632408 is a novel, selective and small-molecule agonist of human and mouse GPR119 with EC50 values of 5.6±0.99 μM and 7.9±0.7 μM, respectively.
M3766 AR-231453 AR-231453 is a potent, selective G-protein coupled receptor 119 (GPR119) agonist (EC50 = 0.68 nM).

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