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. |
| M59165 | Ogremorphin | Ogremorphin (OGM; GPR68-IN-1) is a G protein coupled sensor GPR68 inhibitor, with anti-inflammatory and anti-tumor activities. Ogremorphin can inhibit the migration of human melanoma cells and induce ferroptosis in glioblastoma cells. |
| M55658 | ML-184 | ML-184 (CID2440433) is a selective GPR55 agonist with an EC50 of 250 nM and exhibits >100-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-184(CID2440433) increases proliferation of neural stem cells and promotes neuronal differentiation in vitro. |
| M55197 | CID1231538 | CID1231538 is a potent GPR35 antagonist, with IC50 of 0.55 μM. CID1231538 is a benzothiazole analogue. |
| M38958 | (±)-Pinocembrin | (±)-Pinocembrin ((±)-5,7-Dihydroxyflavanone) is a GPR120 ligand able to promote wound healing in HaCaT cell line. |
| M31033 | BAM(8-22) TFA | BAM(8-22) TFA, a proteolytically cleaved product of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner. |
| 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. |
| M30063 | BAM(8-22) | BAM(8-22), a proteolytically cleaved product of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner. |
| 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. |
| M29193 | (R)-ZINC-3573 | (R)-ZINC-3573 is a selective Mas-related G protein-coupled receptor X2 (MRGPRX2) agonist with an EC50 value of 740 nM. (R)-ZINC-3573 can be used as a MRGPRX2 probe for the research of pain and itch. |
| M25489 | 2-Oleoylglycerol | 2-Oleoylglycerol is a GPR119 agonist, with an EC50 of 2.5 μM for human GPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol stimulates glucagon-like peptide-1 (GLP-1) secretion in vivo. |
| 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). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist. |
| M22361 | TP-024 | TP-024 (FTBMT) is a selective GPR52 agonist with an EC50 of 75 nM. |
| M21601 | Pamoic acid | Pamoic acid is a potent GPR35 agonist with EC50 at 79 nM. Pamoic acid has neuroprotective and anti-inflammatory properties. |
| M20180 | WAY-388798 | WAY-388798 is a agonist of free fatty acid receptor 1 (GPR40) |
| M10682 | TAK-041 | TAK-041 is a first-in-class, selective GPR139 agonist with an EC50 of 22 nM. TAK-041 can be used to study negative symptoms of schizophrenia. |
| M10642 | ML382 | ML382 is a potent and selective MrgX1 (Mas-related G protein-coupled receptor X1, MRGPRX1) positive allosteric modulator with EC50 of 190 nM. |
| 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). |
| 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. |
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