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GPR40 agonists

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By Targets:	GPR84 (5) Bacterial (3) Calcium Channel (1) Endogenous Metabolite (1) Free Fatty Acid Receptor (55) GLP Receptor (1) Potassium Channel (2) PPAR (1) Reference Standards (6)
By Research Areas:	Cardiovascular Disease (5) Endocrinology (2) Infection (2) Inflammation/Immunology (7) Metabolic Disease (55) Neurological Disease (1)

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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-10480

Fasiglifam Maximum Cited Publications 17 Publications Verification TAK-875	Free Fatty Acid Receptor	Metabolic Disease
Fasiglifam (TAK-875) is a potent, selective and orally bioavailable *GPR40* agonist with EC₅₀ of 72 nM.

HY-15589

GW9508 5+ Cited Publications	Free Fatty Acid Receptor Potassium Channel	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
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 .

HY-132265

SCO-267 3 Publications Verification	Free Fatty Acid Receptor	Metabolic Disease
SCO-267 is an allosteric *GPR40* full agonist. SCO-267 can be used for the research of chronic diseases including diabetes .

HY-15697

TUG-770 3 Publications Verification	Free Fatty Acid Receptor	Metabolic Disease
TUG-770 is a potent, selective and orally active *GPR40/FFA1* agonist with an EC₅₀ of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research . TUG-770 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-13467

AM-1638 3 Publications Verification	Free Fatty Acid Receptor	Metabolic Disease
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%) .

HY-B1021

Vincamine 1 Publications Verification	Free Fatty Acid Receptor	Cardiovascular Disease Metabolic Disease
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 .

HY-124571

ZQ-16	GPR84	Inflammation/Immunology
ZQ-16 is a potent and selective GPR84 agonist with an EC₅₀ value of 0.213 μM. ZQ-16 has no activity on the other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119 and GPR120 .

HY-123297

TUG-469	Free Fatty Acid Receptor	Metabolic Disease
TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC₅₀ value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes .

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-100775

Fezagepras sodium 1 Publications Verification Setogepram sodium; PBI-4050 sodium	Free Fatty Acid Receptor GPR84	Metabolic Disease Inflammation/Immunology
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 .

HY-100775A

Fezagepras 1 Publications Verification Setogepram; PBI-4050	Free Fatty Acid Receptor GPR84	Metabolic Disease Inflammation/Immunology
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 .

HY-16619

AM-5262	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-103083

GPR40 agonist 4	Free Fatty Acid Receptor	Metabolic Disease
GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC₅₀ of 7.54.

HY-148418

TUG-499	Free Fatty Acid Receptor	Metabolic Disease
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC₅₀ of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes . TUG-499 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-13967B

AMG 837 calcium hydrate 3 Publications Verification	Bacterial Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-14363

TUG-424	Free Fatty Acid Receptor	Metabolic Disease
TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC₅₀ of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity . TUG-424 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-111763

GPR40/FFAR1 modulator 1	Free Fatty Acid Receptor	Metabolic Disease
GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1) .

HY-147351

GPR40 agonist 6	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-112603

AP5	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-130120

HWL-088	Free Fatty Acid Receptor PPAR	Metabolic Disease
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 .

HY-117787

TUG-905	Free Fatty Acid Receptor	Neurological Disease Metabolic Disease
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 .

HY-13967

AMG 837 3 Publications Verification	Free Fatty Acid Receptor Bacterial	Infection Metabolic Disease
AMG 837 is an orally active, selective *GPR40/FFA1* agonist with an EC₅₀ of 1.5 nM against human *GPR40. AMG 837 stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models . AMG 837 binds to the BacA* protein and impairs the survival and replication of Brucella. AMG 837 can be used in research related to type 2 diabetes and brucellosis .

HY-147420

Xelaglifam IDG-16177	Free Fatty Acid Receptor	Metabolic Disease
Xelaglifam is a potent *GPR40* agonist. Antihyperglycaemic activity . Xelaglifam 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-175420

K-757	GLP Receptor	Metabolic Disease
K-757 is a *GPR40* agonist with an EC₅₀ of 2.1 ± 0.2 nM for human GPR40. K-757 exhibits a half-life of 1-11 h in Preclinical Species. K-757 stimulates GLP-1 secretion and has potential applications in bariatric research .

HY-15589R

GW9508 (Standard)	Free Fatty Acid Receptor Potassium Channel Reference Standards	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
GW9508 (Standard) is the analytical standard of GW9508. This product is intended for research and analytical applications. 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 (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .

HY-W727728

MK-8666	Free Fatty Acid Receptor	Metabolic Disease
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].

HY-177296

GPR40 agonist 8	Free Fatty Acid Receptor Calcium Channel	Metabolic Disease
GPR40 agonist 8 (Compound 2) is a *GPR40* agonist with an EC₅₀ of 5 nM for hGPR40 Ca ²⁺. GPR40 agonist 8 can be used in the research of diseases such as Type II diabetes and obesity .

HY-12585

AM-4668	Free Fatty Acid Receptor	Metabolic Disease
AM-4668 is a *GPR40* agonist for type 2 diabetes. EC₅₀s of 3.6 nM and 36 nM for GPR40 in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), respectively .

HY-141653

MK-8666 tromethamine	Free Fatty Acid Receptor	Metabolic Disease
MK-8666 (tromethamine) is a *GPR40* agonist. MK-8666 (tromethamine) can be used in the research of type II diabetes .

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-147678

GPR40 agonist 5	Free Fatty Acid Receptor	Metabolic Disease
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.

HY-W010655

Fasiglifam hemihydrate TAK-875 hemihydrate	Free Fatty Acid Receptor	Metabolic Disease
Fasiglifam (TAK-875) hemihydrate is a potent, selective and orally active *GPR40* agonist with EC₅₀ of 72 nM. Fasiglifam enhances glucose-dependent insulin secretion and improves hyperglycemia in type 2 diabetic rats. Fasiglifam can induce liver injury .

HY-160602

CPL207280	Free Fatty Acid Receptor	Metabolic Disease
CPL207280 is an orally active *GPR40/FFA1* agonist with an antidiabetic effect. CPL207280 can effectively enhance glucose-stimulated insulin secretion and improve glucose tolerance in MIN6 pancreatic β-cells as well as in healthy Wistar Han rats and diabetic rat models. CPL207280 can be used for the research of type 2 diabetes .

HY-148247

BI-2081	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-108020

LY2881835	Free Fatty Acid Receptor	Endocrinology
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.

HY-U00395

GPR40 Agonist 2	Free Fatty Acid Receptor	Metabolic Disease
GPR40 Agonist 2 is a *GPR40* agonist that can be used in the research of diabetes, extracted from patent WO2009054479A1.

HY-111359

GPR40 agonist 1	Free Fatty Acid Receptor	Metabolic Disease
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.

HY-162136

GPR40 agonist 7	Free Fatty Acid Receptor	Metabolic Disease
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

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-112603A

AP5 sodium	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-13967A

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

HY-111116

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

HY-10480A

(R)-Fasiglifam (R)-TAK-875	Free Fatty Acid Receptor	Metabolic Disease
(R)-Fasiglifam is the isomer of Fasiglifam (HY-10480), and can be used as an experimental control. Fasiglifam (TAK-875) is a potent, selective and orally bioavailable *GPR40* agonist with EC₅₀ of 72 nM.

HY-B1021R

Vincamine (Standard)	Reference Standards Free Fatty Acid Receptor	Cardiovascular Disease Metabolic Disease
Vincamine (Standard) is the analytical standard of Vincamine. This product is intended for research and analytical applications. 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 .

HY-P1124

AS2034178 free base	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-123871

AS2575959 sodium	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-129707

AMG 837 hemicalcium	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-12413A

BMS-986118	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-100775R

Fezagepras sodium (Standard) Setogepram sodium (Standard); PBI-4050 sodium (Standard)	Reference Standards Free Fatty Acid Receptor GPR84	Metabolic Disease Inflammation/Immunology
Fezagepras (sodium) (Standard) is the analytical standard of Fezagepras (sodium). This product is intended for research and analytical applications. 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 .

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GPR40 agonists

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