Free Fatty Acid Receptor Agonist

AS2575959 (sodium) is an agonist of GPR40. AS2575959 (sodium) can enhance glucose metabolism and has synergic effect with Sitagliptin (HY-13749) on insulin as well as incretin secretion. AS2575959 (sodium) can be studied in research on type 2 diabetes.

GPR40 agonist 5 (compound I-14) is an orally active and potent GPR40 (G protein coupled receptor 40) agonist, with an EC₅₀ of 47 nM. GPR40 agonist 5 decreases the levels of blood glucose and improves the glucose tolerance. GPR40 agonist 5 has sufficient effectiveness for the control of hyperglycemia state in type 2 diabetic mice. GPR40 agonist 5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

AM-6226 is a potent and orally active G protein coupled receptor 40 (GPR40) full agonist with an EC₅₀ of 0.12 μM. AM-6226 can activate the GPR40 receptors on pancreatic β cells and enteroendocrine L cells, promote insulin secretion in a glucose-dependent manner and also increase the release of incretin hormones (GLP-1, GIP), thereby avoiding the risk of hypoglycemia. AM-6226 can be used for the research of metabolic disease, such as diabetes.

GPR43 agonist 1 is a selective, orally active GPR43 agonist. GPR43 agonist 1 downregulates the activity of NF-κB. GPR43 agonist 1 can be used in studies of acute colitis.

GPR40 agonist 7 (Compound 1) is an orally active G protein-coupled receptor 40 (GPR40) agonist. GPR40 agonist 7 can significantly increase insulin and GLP-1 secretion, and has a hypoglycemic effect in vivo with an ED₅₀ of 0.58 mg/kg

MK-8666 (tromethamine) is a GPR40 agonist. MK-8666 (tromethamine) can be used in the research of type II diabetes.

(rel)-AM-6226 is the relative stereoisomer of AM-6226 (HY-120493A). AM-6226 is a potent, orally active full agonist of G protein-coupled receptor 40 (GPR40) with an EC₅₀ value of 0.12 μM. AM-6226 activates GPR40 receptors on pancreatic β-cells and enteroendocrine L-cells, promotes insulin secretion in a glucose-dependent manner, and increases the release of incretin hormones (GLP-1, GIP), thus avoiding the risk of hypoglycemia. AM-6226 can be used in the research of metabolic diseases such as diabetes.

FFAR1/FFAR4 agonist-1 (compound 83) is a FFAR1/FFAR4 agonist with the EC₅₀ of 1 nM A and 4nM for FFAR1 and FFAR4, respectively. FFAR1/FFAR4 agonist-1 can be used for study of glycemic control.

Phytosphingosine-d₇ (4-Hydroxysphinganine-d₇) is deuterium labeled Phytosphingosine. 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.

GPR40 agonist 9 (Example 21) is a G protein-coupled receptor 40 (GPR40) agonist with an EC₅₀ of 0.21 nM. GPR40 agonist 9 is applicable to research related to type 2 diabetes, obesity, and other associated conditions.

BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC₅₀ of 0.07 µM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models.

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

AS2034178 free base, a specific and orally active GPR40 agonist, exhibits glucose-dependent insulin secretion enhancement. AS2034178 free base has potential for type 2 diabetes mellitus research.

LXT34 (Example 2) is a GPR120 agonist. LXT34 has an anti-inflammatory activity. LXT34 promotes GLP-1 formation in the gastrointestinal tract and improves insulin resistance in macrophages and pancreas cells. LXT34 can be used for inflammatory diseases, such as type 2 diabetes, obesity and non-alcoholic fatty liver research.

FFA1 agonist-1 (Compound 17a) is an orally active fatty acid receptor 1 (FFA1) agonist with an EC₅₀ of 0.75 μM. FFA1 agonist-1 can be used for type 2 diabetes mellitus research.

GPR40 agonist 8 (Compound 2) is a GPR40 agonist with an EC₅₀ of 5 nM for hGPR40 Ca²⁺. GPR40 agonist 8 can be used in the research of diseases such as Type II diabetes and obesity.

LY2881835 is a potent and selective agonist of G protein-coupled receptor 40 (GPR40). LY2881835 has efficacious and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion. LY2881835 has the potential for the research of type 2 diabetes mellitus. LY2881835 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Metabolex-36 is a FFA4 agonist with a pEC₅₀ value of 5.9 and a pEC₅₀ value of less than 4.0 for FFA1.

FFAR4 agonist-1 is an orally active, selective agonist of FFAR4. FFAR4 agonist-1 improves glucose tolerance, reduces blood glucose levels and promotes insulin secretion. FFAR4 agonist-1 can be used in the research of type 2 diabetes.

FFA2 agonist-2 is a potent agonist of the FFA2 (GPR43) receptor, with a pEC₅₀ of 7.9 for human FFA2, and a pEC₅₀ of 7.3 for murine FFA2. FFA2 agonist-2 acts as an orthosteric agonist and shows no obvious cross‑activity against FFA1, FFA3 and FFA4. FFA2 agonist-2 can be used for FFA2 receptor research in type 2 diabetes and metabolic disorders.