free fatty acid receptor

TUG-891 is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

Vincamine (Perval) is a major alkaloid of Vinca minor L., Apocynaceae. It has been used therapeutically as a vasodilator and antihypertensive agent, particularly in cerebrovascular disorders.

(2S,3R,4S)-4-Hydroxyisoleucine (Hydroxyisoleucine) from fenugreek (Trigonella foenum-graecum) seeds is a potential insulinotropic (anti-diabetic) and anti-obesity amino acid that stimulates glucose-dependent insulin secretion from pancreatic cells, activates insulin receptor substrate-associated phosphoinositide 3 (PI3) kinase activity, and reduces plasma levels of triglycerides, free fatty acids, and cholesterol.

4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).

TUG-1375 is an Agonist of Thiazolidine Free Fatty Acid Receptor 2

GSK137647A (GSK 137647) is a selective agonist of FFA4.

GW9508(GW 9508) is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.

Ginsenoside Rb2 (Ginsenoside C) found in species of Panax, upregulating GPR120 gene expression.

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist (EC50: 7.39). It shows higher affinity for FFAR1 or GPR40 relative to related receptors FFA2, FFA3, and the nuclear receptor PPARγ, as well as various other receptors, ion channels, and transporter proteins. TUG-499 is useful for studying Type 2 diabetes.

GPR120 Agonist 2 is a potent and selective GPR120 receptor agonist.

(+ -)-Pinocembrin (NSC-43318), a natural product from axillary pines, is a GPR120 ligand that promotes wound healing in the HaCaT cell line.

GPR40 FFAR1 modulator 1 is a Gq-coupled free fatty acid receptor 1 (GPR40 FFAR1) agonist and allosteric modulator.

Spexin acetate is a potent galanin receptor 2 3 (GAL2 GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Exhibits no significant activity at galanin receptor 1. Endogenous satiety-inducing peptide; inhibits long chain fatty acid uptake by ad

TUG-469 is an agonist of free fatty acid 1(FFA) receptor.

GPR120 Agonist 3 (GPR120-IN-1) is a selective agonist of Gpr120 ( logEC50: -7.62).

GprA, a novel synthetic agonist for G Protein-Coupled Receptor 120 Free Fatty Acid Receptor 4 (GPR120 FFAR4), demonstrates an AC50 of 203 nM on the full-length human GPR120 isoform. It is valuable for research into non-alcoholic fatty liver disease (NAFLD).

TUG-905 is an agonist for free fatty acid receptor 4 (FFA4/GPR120), and TUG-905 has the potential to treat agitation.

ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic steatosis and plasma alanine transaminase (ALT) and aspartate aminotransferase (AST) levels in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a methionine and choline-deficient diet at the same dose. 1.Li, Z., Chen, Y., Zhou, Z., et al.Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agentsEur. J. Med. Chem.164352-365(2019) 2.Li, Z., Zhou, Z., Hu, L., et al.ZLY032, the first-in-class dual FFA1/PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosisPharmacol Res.159105035(2020)

3-chloro-5-hydroxy Benzoic Acid (3-chloro-5-hydroxy BA) is an agonist of GPR81 (EC50 : 16 μM)

AH-7614 (AH 7614) is a selective and potent free fatty acid receptor 4 (FFA4 GPR120) antagonist.

1-methoxycyclopropanecarboxylic acid is an agonist of free fatty acid receptor 3 (FFAR3, human).

Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 |Zhang et al (2016) Discovery and characterization of a novel small-molecule agonist for medium-chain free fatty acid receptor G protein-coupled receptor 84. J.Pharmacol.Exp.Ther. 357 337 PMID:26962172

E-3030 free acid is a peroxisome proliferator-activated receptor (PPAR) agonist. E-3030 decreased blood glucose, triglyceride, non-esterified fatty acids, and insulin levels and increased blood adiponectin levels. Triglyceride- and non-high-density lipopr