Free Fatty Acid Receptor Agonist

GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate.

GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC₅₀ of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.

Phytosphingosine (Standard) is the analytical standard of Phytosphingosine. This product is intended for research and analytical applications. 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[1][2][3][4].

LY3104607 is a potent and selective G protein-coupled receptor 40 (GPR40) agonist. LY3104607 can be used in research of diabetes.

AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 demonstrates rat and human inositol monophosphate (IP1) EC₅₀ values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 has the potential for type II diabetes research.

BI-2081, a chemical probe, is a GPR40 (FFAR1) partial agonist (EC₅₀: 4 nM). BI-2081 induces glucose depending insulin secretion and reduces the plasma glucose concentration. BI-2081 can be used in the research of metabolic diseases, in particular diabetes type 2.

AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [³H]AMG 837 binding at the human FFA1 receptor with a pIC₅₀ of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.

AM-5262 is a GPR40 full agonist with an EC₅₀ value of 0.081 μM. AM-5262 can be used for the research of type II diabetes.

MK-8666 is a potent and selective partial GPR40 agonist (EC₅₀ = 0.54 nM for human GPR40). MK-8666 shows selectivity over GPR119, GPR43, GPR41, GPR120, and other G-protein-coupled receptors (GPCRs). MK-8666 reduces glucose in the rodent. MK-8666 can be used for type 2 diabetes research^[1][2].

Tacrine (hydrochloride) (Standard) is the analytical standard of Tacrine (hydrochloride). This product is intended for research and analytical applications. Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease.

TP-051, a chemical probe, is a potent FFAR1 agonist with an K_i 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.

Tiglic acid (Standard) is the analytical standard of Tiglic acid (HY-W012999). This product is intended for research and analytical applications. Tiglic acid is a monocarboxylic unsaturated organic acid. Tiglic acid can be isolated from croton oil. Tiglic acid agonizes FFA2 and upregulates PYY expression. Tiglic acid derivatives have anti-inflammatory activity. Tiglic acid can be used in the research of obesity, diabetes, and inflammatory diseases.

TUG-905 is a potent GPR40 agonist with an pEC₅₀ value of 7.03. TUG-905 increases hypothalamic cell proliferation and survival. TUG-905 reduces body mass and increases the POMC mRNA expression.

GPR120 Agonist 5 (compound 12) is an agonist targeting GPR120 (EC₅₀=1.2 μM). GPR120 Agonist 5 promotes the release of glucagon-like 1 (GLP-1) by binding to the GPR120 receptor, which in turn binds to its receptors on pancreatic beta cells, increasing insulin secretion and thereby lowering blood sugar levels. GPR120 Agonist 5 also helps reduce chronic low-grade inflammation, which plays an important role in the pathogenesis of obesity, insulin resistance, and type 2 diabetes. GPR120 Agonist 5 can be used to investigate the mechanism of action of GPR120 in metabolic and inflammatory diseases.

FFA2 agonist-1 (Compound 4) is the agonist for Free fatty acid receptor 2 (FFA2/GPR43) with an EC₅₀ of 81 nM. FFA2 agonist-1 exhibits activity in β-arrestin-2 recruitment assay and cAMP inhibition assay with EC₅₀ of 1.2 μM and 0.53 μM. FFA2 agonist-1 leads to appetite regulating peptide YY (PYY) mucosal responses, inhibits the fat accumulation, intestinal functions and food intake, and can be used for obesity research.

K-757 is an orally active, gut-targeted GPR40 agonist with EC₅₀ values of 2.1 nM, 5.6 nM, 4.2 nM and 166 nM in humans, mice, rats and dogs, respectively. K-757 activates nutrient receptors co-expressed on pancreatic β cells and intestinal enteroendocrine cells. K-757 mediates and induces the secretion of satiety hormones GLP-1 and PYY in multiple in vitro and in vivo models. When used in combination with GPR119 agonist K-833, K-757 acts as a potentiator to elevate circulating levels of satiety hormones. K-757 can be used in the research of type 2 diabetes, weight loss and other related metabolic disorders.

MK-2305 is an orally active GPR40 partial agonist with an EC₅₀ of 6 nM in rats. MK-2305 mediates glucose-stimulated insulin secretion and inhibits endogenous glucose production by reducing gluconeogenesis from tricarboxylic acid (TCA) cycle substrates. MK-2305 increases plasma insulin levels under hyperglycemic and glucose-stimulated conditions, reduces fasting blood glucose, and improves glucose homeostasis. MK-2305 can be used in studies related to type 2 diabetes.

GPR120 Agonist 4 (example 1) is a GPR120 agonist，with the EC₅₀ values of 1 μM and 0.35 μM for β-arrestin A and Calcium A. GPR120 Agonist 4 can be used for the research of type II diabetes mellitus.

(R)-AM-1638 is a R-isomer of AM-1638 (HY-13467). AM-1638 is an orally active full agonist of GPR40 (EC₅₀: 0.16 μM).

GprA is a new synthetic agonist of G-protein-coupled receptor 120/free fatty acid receptor 4 (GPR120/FFAR4), with an AC₅₀ of 203 nM on human GPR120 full isoform. GprA can be used in the research for NAFLD.