Inhibitor/Activator
| Cat.No. | Name | Information |
|---|---|---|
| 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. |
| M29734 | PW0787 | PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior. |
| M29553 | MS48107 | MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice. |
| M29415 | RTI-13951-33 | RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats. |
| M29237 | GPR40 agonist 4 | GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54. |
| M28869 | (S)-CVN424 | (S)-CVN424 is a potent G-Protein-Coupled Receptor 6 (GPR6) modulator. (S)-CVN424 has the potential for a variety of neurological and psychiatric disorders research, including Parkinson's disease. |
| M28762 | GRK5-IN-2 | GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research. |
| M28672 | BMS-986118 | BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC50 of 0.07 µM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models. |
| M28651 | ML401 | ML401, a potent chemical probe, selectively antagonizes EBI2 (also known as GPR183) with an IC50 of 1.03 nM. ML401 displays activity in a chemotaxis assay (IC50=6.24 nM). ML401 shows good stability and no toxicity. |
| M28493 | BI-2081 | BI-2081 is a GPR40 (FFAR1) partial agonist (EC50: 4 nM). BI-2081 induces glucose depending insulin secretion and reduces the plasma glucose concentration. BI-2081 can be used in the research of metabolic diseases, in particular diabetes type 2. |
| M28369 | TC-G 1005 | TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo. |
| M28272 | Firuglipel | Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist. |
| M28122 | LY2881835 | LY2881835 is a potent and selective agonist of G protein-coupled receptor 40 (GPR40). LY2881835 has efficacious and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion. LY2881835 has the potential for the research of type 2 diabetes mellitus. |
| M28079 | AMG 837 calcium hydrate | AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents. |
| M28051 | Fezagepras sodium | Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras sodium decreases renal, liver and pancreatic fibrosis. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions. |
| M28005 | GPR120 Agonist 2 | GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209. |
| M27673 | GSK2041706A | GSK2041706A (GSK706) is a potent G protein-coupled receptor 119 (GPR119) agonist. GSK2041706A can be used for the research of type 2 diabetes. |
| M27599 | Fezagepras | Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras decreases renal, liver and pancreatic fibrosis. Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions. |
| M21826 | AM-1638 | AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM. |
| M6468 | AS 2034178 | AS 2034178 is a selective FFA1 (GPR40) agonist. |
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