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GPR40 Activator

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By Targets:	ERK (1) Free Fatty Acid Receptor (9) HDAC (1) Microtubule/Tubulin (1)
By Research Areas:	Endocrinology (1) Metabolic Disease (7) Neurological Disease (1)

Targets Recommended: GPR39 G2A (GPR132) EBI2/GPR183 GPR84 Kisspeptin Receptor Succinate Receptor 1 GPR55 GPR88 GPR171 GPR35 GPR119 GPR4 GPR139 GPR6 GPR65 GPR52 GPR68 GPR109A MCHR1 (GPR24) CX3CR1 Neuropeptide S Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19835

LY2922470	Free Fatty Acid Receptor	Metabolic Disease
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) .

HY-12647

GPR40 Activator 2	Free Fatty Acid Receptor	Metabolic Disease
GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.

HY-172944

GPR40 Activator 3	Free Fatty Acid Receptor	Metabolic Disease
GPR40 Activator 3 (compound SC) is a potent *GPR40* activator. GPR40 Activator 3 mitigates pulmonary fibrosis by inhibiting M2 macrophage polarization via the GPR40/PKD1/CD36 axis .

HY-13971

GPR40 Activator 1	Free Fatty Acid Receptor	Metabolic Disease
GPR40 Activator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-111141

AM-3189	Free Fatty Acid Receptor	Metabolic Disease
AM-3189 is an orally active and selective *GPR40* agonist with EC₅₀ values in buffer solution and in 100% human serum of 33 nM and 10 μM respectively. AM-3189 shows no significant activity on GPR41 and GPR43, and no agonistic activity on PPAR-α, -δ, and -γ. AM-3189 enhances glucose-stimulated insulin secretion by activating GPR40 on pancreatic β cells. AM-3189 has extremely low penetration into the central nervous system and significantly reduces blood glucose levels in two humanized GPR40 mouse models. AM-3189 can be used for the study of type 2 diabetes .

HY-120493A

AM-6226	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-176733

HDAC6-IN-61	HDAC Free Fatty Acid Receptor Microtubule/Tubulin ERK	Neurological Disease
HDAC6-IN-61 (Compound 4e) is a HDAC6 inhibitor (IC₅₀: 73 nM) with selectivity over other HDAC isoforms. HDAC6-IN-61 is also a *GPR40* activator. HDAC6-IN-61 increases acetylated tubulin and ERK phosphorylation levels. HDAC6-IN-61 can be used for research of neuroinflammation such as Alzheimer's disease .

HY-117978

LY2922083	Free Fatty Acid Receptor	Endocrinology
LY2922083 and related compounds LY2881835 and LY2922470 are spiperidine and tetrahydroquinolinic acid derivatives that are potent GPR40 agonists. LY2922083 activates GPR40 in response to elevated blood glucose and has the potential to be a glucose-lowering agent .

HY-120493

(rel)-AM-6226	Free Fatty Acid Receptor	Metabolic Disease
(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 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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GPR40 Activator

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