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. |
| M45110 | GSK4381406 | GSK4381406 is a first-in-class, orally active GPR35 agonist for studies related to inflammatory bowel disease (IBD). |
| M41868 | hMCH-1R antagonist 1 | hMCH-1R antagonist 1 is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. |
| M41851 | Kisspeptin 234 | Kisspeptin 234, is a 10 amino acid peptide as well as a kisspeptin receptor (KISS1, GPR54) antagonist. |
| M41850 | Kisspeptin 234 TFA | Kisspeptin 234 TFA, is a 10 amino acid peptide as well as a kisspeptin receptor (KISS1, GPR54) antagonist. |
| M41842 | Bufrolin | Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. |
| M41841 | GPR119 agonist 2 | GPR119 agonist 2 is an orally active GPR119 agonist. |
| M41840 | GPCR agonist-2 | GPCR agonist-2 is a GPCR GPR109b (HM74) agonist, with a pEC50 value of 6.51. |
| M41821 | AM-5262 | AM-5262 is a GPR40 full agonist with an EC50 value of 0.081 μM. |
| 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. |
| 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. |
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