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GPR/FFAR G protein-coupled receptor/Free fatty acid receptors

Inhibitor/Activator

Cat.No.  Name Information
M55197 CID1231538 CID1231538 is a potent GPR35 antagonist, with IC50 of 0.55 μM. CID1231538 is a benzothiazole analogue.
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.
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.
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 FTBMT FTBMT (TP-024) 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.
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).
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.
M8281 4-CMTB 4-CMTB is a potent allosteric agonist of free fatty acid receptor 2 (FFA2).
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.
M6985 Monomethyl fumarate MMF is a activator of Nrf2 pathway; primary metabolite of DMF.
M6849 JNJ 63533054 JNJ-63533054 is a potent, selective, orally active GPR139 agonist.JNJ-63533054 is more selective for GPR139 than other GPCR, ion channel and transporter proteins.JNJ-63533054 can cross the blood-brain barrier (BBB).
M6466 AS 1269574 AS1269574 is a potent, orally active GPR119 agonist with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates the TRPA1 cation channel and stimulates glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induced pancreatic β cells to secrete glucose-dependent insulin only under high glucose conditions. AS1269574 has potential for type 2 diabetes research.




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