Free Fatty Acid Receptor Agonist

Phytosphingosine is a phospholipid with anti-inflammatory, antibacterial, and anti-cancer activities, which can induce apoptosis. Phytosphingosine is an immune regulator and can be used in the study of inflammatory skin diseases. Phytosphingosine is also an activator of GPR120 with an IC₅₀ value of 33.4 μM and can be used in the study of type II diabetes.

TUG-891 is a potent and selective agonist for the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120).

3-Amino-3-(p-tolyl) propionic acid (3-Amino-3-(4-methylphenyl) propanoic acid) is a GPR40 agonist. 3-Amino-3-(p-tolyl) propionic acid is used for research on type 2 diabetes, obesity, metabolic syndrome and lipid disorders.

GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC₅₀s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (K_ATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.

AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC₅₀=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca²⁺ signal-mediated glucose uptake and improve diabetes.

AM-1638 is an orally active full agonist of GPR40 (EC₅₀: 0.16 μM). AM-1638 increases the expression of antioxidant molecules (HO-1 and NQO-1). AM1638 blocks Palmitate (HY-N0830)-mediated superoxide production and ER stress. AM-1638 has antidiabetic activity and improves glycemic control in BDF mice with diet-induced obesity (DIO). AM-1638 demonstrates excellent oral bioavailability (mouse, >100%; rat, 72%; and cyno, 71%).

SCO-267 is an allosteric GPR40 full agonist. SCO-267 can be used for the research of chronic diseases including diabetes.

Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras decreases renal, liver and pancreatic fibrosis. Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.

Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation. Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research.

Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras sodium decreases renal, liver and pancreatic fibrosis. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.

AMG7703 is a selective and allosteric agonists of FFA2 (GPR43), the receptor for short-chain fatty acids (SCFAs), acetate, and propionate. AMG7703 can be used to research for in inflammatory and metabolic.

AMG 837 calcium hydrate is an orally active, selective GPR40/FFA1 agonist with an EC₅₀ of 1.5 nM against human GPR40. AMG 837 calcium hydrate stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models. AMG 837 calcium hydrate binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 calcium hydrate can be used in research related to type 2 diabetes and brucellosis.

13Z,16Z-Docosadienoic acid is a GPR120 agonist with bactericidal activity. 13Z,16Z-Docosadienoic acid serves as a potential biomarker for canine mammary tumors. 13Z,16Z-Docosadienoic acid is used in the research of bacterial infections, Lyme disease, Graves' disease and mammary tumors.

Tricosanoic acid is an endogenous agonist of long-chain saturated fatty acids and free fatty acid receptor FFAR1, which can activate hair growth. Tricosanoic acid (C23:0) has the activity of improving cognitive function by regulating neuronal membrane fluidity, inhibiting neuroinflammatory response, participating in myelination and neuronal energy metabolism. Tricosanoic acid expression levels are low in the prefrontal cortex of Alzheimer's disease (AD) models; while better cognitive performance corresponds to higher serum concentration levels. Tricosanoic acid can be used as a biomarker for diseases related to cognitive decline.

GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC₅₀ of 7.62.

GPR40 agonist 6 (Compound 7a) is a potent and selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist with an EC₅₀ of 0.058 μM.

GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC₅₀ values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC₅₀ values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response.

GPR41 agonist-1 (compound 9) is a potent GPR41 agonist. GPR41 agonist-1 can be used for researching insulin-related disorders.

LY2922470 is a selective and orally active agonist for the G protein-coupled receptor 40 (GPR40). LY2922470 activates GPR40-mediated β-arrestin recruitment with EC₅₀s of 7 nM (human GPR40), 1 nM (mouse GPR40) and 3 nM (rat GPR40). LY2922470 can be used for research of type 2 diabetes mellitus (T2DM).

HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC₅₀ of 18.9 nM) with moderate PPARδ activity (EC₅₀ of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.