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Isoforms Recommended:	FFAR1

Results for "

GPR40

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GPR119 (1) GPR84 (5) Apoptosis (2) Bacterial (3) Calcium Channel (1) Dipeptidyl Peptidase (1) Endogenous Metabolite (1) ERK (1) Free Fatty Acid Receptor (63) GLP Receptor (1) HDAC (1) Microtubule/Tubulin (1) Potassium Channel (2) PPAR (1) Reference Standards (7) Small Interfering RNA (siRNA) (3)
By Research Areas:	Cardiovascular Disease (5) Endocrinology (2) Infection (2) Inflammation/Immunology (8) Metabolic Disease (63) Neurological Disease (2)
Oligonucleotides:	Rat Pre-designed siRNA Sets (1) Mouse Pre-designed siRNA Sets (1) Human Pre-designed siRNA Sets (1) siRNAs (3)

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Natural
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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 15+ 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-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-50691

GW-1100 Maximum Cited Publications 21 Publications Verification	Free Fatty Acid Receptor	Metabolic Disease
GW-1100 is a selective *GPR40* antagonist with a pIC₅₀ of 6.9.

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-101906

DC260126 3 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-160631

GPR40 agonist 9	Free Fatty Acid Receptor	Metabolic Disease
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 .

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-103083R

GPR40 agonist 4 (Standard)	Reference Standards Free Fatty Acid Receptor	Metabolic Disease
GPR40 agonist 4 (Standard) is the analytical standard of GPR40 agonist 4 (HY-103083). This product is intended for research and analytical applications. GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC₅₀ of 7.54.

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-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-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-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-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-50691R

GW-1100 (Standard)	Free Fatty Acid Receptor	Metabolic Disease
GW-1100 (Standard) is the analytical standard of GW-1100. This product is intended for research and analytical applications. GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.

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-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-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-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-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-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-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 .

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