Inhibitor/Activator
| Cat.No. | Name | Information |
|---|---|---|
| M30771 | GPR35 agonist 4 | 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. |
| M30741 | AMG 837 sodium salt | AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. |
| M30736 | GSK299115A | GSK299115A is a G Protein-coupled Receptor Kinase (GRK) and PKA inhibitor. |
| M30725 | MCHR1 antagonist 2 | MCHR1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHR1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells. |
| M30711 | TP-051 | TP-051 is a potent FFAR1 agonist with an Ki value of 16 nM for human FFAR1. TP-051 can increase insulin secretion in rat insulinoma cells. TP-051 can be used to research type 2 diabetes. |
| M30428 | 7α,25-Dihydroxycholesterol | 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells. |
| M30395 | 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). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist. |
| M30163 | SNAP 94847 | SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters. |
| M30142 | NGD-4715 | NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist . |
| M30107 | TC-O 9311 | TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM. |
| M29944 | NCRW0005-F05 | NCRW0005-F05 is a potent GPR139 antagonist with an IC50 value of 0.21 μM. NCRW0005-F05 can be used to research diabetes, obesity and Parkinson's disease. |
| 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. |
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