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Results for "

GPR40

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) ATP Citrate Lyase (1) Free Fatty Acid Receptor (39) GPR84 (2) Potassium Channel (1) PPAR (1)
By Research Areas:	Cardiovascular Disease (2) Endocrinology (1) Inflammation/Immunology (3) Metabolic Disease (39) Neurological Disease (1)

Inhibitors & Agonists

Natural
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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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.

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-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-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.

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-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.

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-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-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-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-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-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-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-19835

LY2922470	Free Fatty Acid Receptor	Metabolic Disease
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC₅₀s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM) .

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-160602

CPL207280

Free Fatty Acid Receptor Metabolic Disease

CPL207280 is an orally active GPR40/FFA1 agonist with anti-diabetic effects .

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 .

CPL207280	Free Fatty Acid Receptor	Metabolic Disease
CPL207280 is an orally active GPR40/FFA1 agonist with anti-diabetic effects .

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-13467

AM-1638

1 Publications Verification

Free Fatty Acid Receptor Metabolic Disease

AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC₅₀ of 0.16 μM.

AM-1638 1 Publications Verification	Free Fatty Acid Receptor	Metabolic Disease
AM-1638 is a potent and orally bioavailable *GPR40/FFA1* full agonist with an EC₅₀ of 0.16 μM.

HY-15589

GW9508 4 Publications Verification	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-50691

GW-1100

Maximum Cited Publications

17 Publications Verification

Free Fatty Acid Receptor Metabolic Disease

GW-1100 is a selective GPR40 antagonist with a pIC₅₀ of 6.9.

GW-1100 Maximum Cited Publications 17 Publications Verification	Free Fatty Acid Receptor	Metabolic Disease
GW-1100 is a selective *GPR40* antagonist with a pIC₅₀ of 6.9.

HY-10480

Fasiglifam 10+ Cited Publications 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-101906

DC260126 2 Publications Verification	Free Fatty Acid Receptor Apoptosis	Metabolic Disease
DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca ²⁺ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC₅₀: 6.28, 5.96, 7.07, 4.58 μM, respectively) . DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis .

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-13967B

AMG 837 calcium hydrate 1 Publications Verification	Free Fatty Acid Receptor	Metabolic Disease
AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of *GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [ ³H]AMG 837 binding at the human FFA1 receptor with a pIC₅₀* of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents . AMG 837 (calcium hydrate) 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-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-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	Others	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-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-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-100775

Fezagepras sodium Setogepram sodium; PBI-4050 sodium
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 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-P1123

MEDICA16	ATP Citrate Lyase Free Fatty Acid Receptor	Metabolic Disease
MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for *GPR40* as well as selective partial agonists for *GPR120* .

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-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-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-B1021

Vincamine	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-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-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-148247

BI-2081	Free Fatty Acid Receptor	Metabolic Disease
BI-2081 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-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-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-15697

TUG-770 2 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.

Vincamine	Apocynaceae Cardiovascular Disease Alkaloids Structural Classification Classification of Application Fields Source classification Plants Disease Research Fields Indole Alkaloids Catharanthus roseus (L.) G. Don	Free Fatty Acid Receptor
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 .

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Inhibitors & Agonists

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