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FFA1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenosine Receptor (1) Free Fatty Acid Receptor (14) Potassium Channel (1) PPAR (1)
By Research Areas:	Cardiovascular Disease (2) Inflammation/Immunology (1) Metabolic Disease (15)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 ^[1]. 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.

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 ^[1] . 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.

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 ^[1] .

AM-1638 2 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.

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 ^[1] .

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.

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 ^[1]. 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.

FFA1 agonist-1	Free Fatty Acid Receptor	Metabolic Disease
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 ^[1].

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 ^[1] .

ZLY032	Others	Others
ZLY032 is a dual FFA1/PPARδ agonist with the activity of improving glucose and lipid metabolism, alleviating liver fibrosis, and potentially inhibiting metabolic disorders.

GW9508 5 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 ^[1] .

GSK137647A 1 Publications Verification GSK 137647	Free Fatty Acid Receptor	Metabolic Disease
GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC₅₀ values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC₅₀ values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response ^[1] .

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 ^[1] .

AH-7614 2 Publications Verification	Free Fatty Acid Receptor	Metabolic Disease
AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC₅₀s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC₅₀<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist ^[1] .

Metabolex-36 Met-36	Others	Others
Metabolex-36 is a FFA4 agonist developed by Metabolex (now Cymabay Therapeutics) and used in multiple studies to investigate the function of FFA4. Metabolex-36 was used in conjunction with AstraZeneca compounds (AZ-423 and AZ-670) to investigate FFA4 function in pancreatic delta cells. Metabolex-36 has a pEC50 of 5.9 for FFA4 and a pEC50 of less than 4.0 for FFA1. Compound B was used to investigate the role of FFA4 in growth hormone-releasing peptide (ghrelin) secretion and somatostatin release and was used with FFA4 KO mice. Compound B had an EC50 of 15 nM for FFA4 in an IP3 accumulation assay in FFA4-transfected COS7 cells and was up to 1000-fold selective for FFA1. Compound B inhibited baseline ghrelin secretion from primary gastric mucosal cells but had no effect on cells from FFA4 KO mice. Oral administration of Compound B reduced plasma ghrelin levels in mice under starvation conditions. Compound B also inhibited somatostatin release from primary gastric epithelial cells but had no effect on cells from FFA4 KO mice.

GS-9667 CVT 3619	Adenosine Receptor	Cardiovascular Disease Metabolic Disease
GS-9667 (CVT 3619), a novel N ⁶-5'-substituted adenosine analog, is a selective, partial agonist of the A₁ adenosine receptor (A₁AdoR). GS-9667 binds to adipocyte membranes with high (K_H=14 nM) and low (K_L=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC₅₀ values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA) .

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 ^[1]. 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.

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