GPR40 (Free fatty acid receptor 1, FFA1) is a class A G-protein coupled receptor that in humans is encoded by the FFAR1 gene. It is strongly expressed in the cells of the pancreas and to a lesser extent in the brain. This membrane protein binds free fatty acids, acting as a nutrient sensor for regulating energy homeostasis. GPR40 is activated by medium to long chain fatty acids. GPR40 is most strongly activated by eicosatrienoic acid, but has been found to be activated by fatty acids as small as 10 carbons long. For saturated fatty acids the level of activation is dependent on the length of the carbon chain, which is not true for unsaturated fatty acids. It has been found that three hydrophilic residues (arginine-183, asparagine-244, and arginine-258) anchor the carboxylate group of a fatty acid, which activates GPR40.


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BI-2081

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[1].

  • CAS Number: 1458656-71-7
  • MF: C32H35FO6
  • MW: 534.62
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TUG-499

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[1].

  • CAS Number: 1206629-08-4
  • MF: C16H11Cl2NO2
  • MW: 320.17
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LY3104607

LY3104607 (LY-3104607) is a potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM; demonstrates functional potency and glucose dependent insulin secretion in primary islets from rats; dose-dependently reduces glucose levels in vivo.

  • CAS Number: 1795232-22-2
  • MF: C27H25N3O3
  • MW: 439.515
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AS 2034178

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[1].

  • CAS Number: 1030846-42-4
  • MF: C27H29FN2O3
  • MW: 448.52900
  • Catalog: GPR40
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 657.9±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 351.7±31.5 °C

FAA1 agonist-1

FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.

  • CAS Number: 2102196-57-4
  • MF: C21H17ClO5S
  • MW: 416.87
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PBI-4050

Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis[1][2]. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].

  • CAS Number: 1002101-19-0
  • MF: C13H18O2
  • MW: 206.28100
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMG7703

AMG7703 (4-CMTB, AMG-7703) is an allosteric, selective agonist of FFAR2 (GPR43).

  • CAS Number: 1103523-24-5
  • MF: C14H15ClN2OS
  • MW: 294.800
  • Catalog: GPR40
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TUG-469

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][2].

  • CAS Number: 1236109-67-3
  • MF: C23H23NO2
  • MW: 345.434
  • Catalog: GPR40
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 532.7±38.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 275.9±26.8 °C

LY2881835

A potent, selective, orally available GPR40 agonist with EC50 of 8 nM; displays no activity against PPARα/β/γ (>10 uM); demonstrates potent, efficacious, and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion in vivo.

  • CAS Number: 1292290-38-0
  • MF: C33H33NO3
  • MW: 491.620
  • Catalog: GPR40
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 676.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 363.0±31.5 °C

TP-051

TP-051 is a potent FFAR1 agonist with an Ki value of 16 nM for human FFAR1. TP-051 can increase insulin secretion in rat insulinoma cells. TP-051 can be used to research type 2 diabetes[1].

  • CAS Number: 858097-86-6
  • MF: C29H31FO6S
  • MW: 526.62
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMG 837

AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.IC50 value: 13 nM (EC50) [1]Target: GPR40 agonistAMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showedno significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potentand selective in vitro.

  • CAS Number: 865231-46-5
  • MF: C26H21F3O3
  • MW: 438.43800
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMG 837 (sodium salt)

AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.IC50 value: 13 nM (EC50) [1]Target: GPR40 agonistAMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showedno significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potentand selective in vitro.

  • CAS Number: 865231-45-4
  • MF: C26H20F3NaO3
  • MW: 460.42
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GPR40 agonist 5

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].

  • CAS Number: 2443384-60-7
  • MF: C27H24N2O4
  • MW: 440.49
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TUG-770

TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.IC50 Value: 6 nM (hFFA1, EC50) [1]Target: GPR40in vitro: TUG-770 (Compound 22) displayed excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 furthermore showed excellent stability toward human liver microsomes (HLM), no inhibition of selected CYP-enzymes implicated in drug-drug interactions, no P-glycoprotein (P-gp) inhibition, and good permeability in the Caco-2 cell assay [1].in vivo: Examination of TUG-770 in an acute intraperitoneal glucose tolerance test (IPGTT) in normal mice revealed a good dose dependent response with maximal reduction in glucose level reached at 50 mg/kg. The effect of TUG-770 was fully sustained after 29 days of daily oral treatment. Additional evaluation of TUG-770 in rats confirmed a significant glucose lowering effect for the high doses already after 10 min and for all doses after 30 min [1].Clinical trial:

  • CAS Number: 1402601-82-4
  • MF: C19H14FNO2
  • MW: 307.318
  • Catalog: GPR40
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 523.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 270.4±30.1 °C

GPR40/FFAR1 modulator 1

GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1)[1].

  • CAS Number: 874755-26-7
  • MF: C21H19N5O3
  • MW: 389.41
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TUG-905

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[1][2].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GPR40 Agonist 2

GPR40 Agonist 2 is a GPR40 agonist that can be used in the research of diabetes, extracted from patent WO2009054479A1.

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AP5 sodium

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[1].

  • CAS Number: 1623143-67-8
  • MF: C28H27FNNaO4
  • MW: 483.51
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Xelaglifam

Xelaglifam is a potent GPR40 agonist. Antihyperglycaemic activity[1].

  • CAS Number: 2230597-99-4
  • MF: C30H28FNO5
  • MW: 501.55
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GPR40 Activator 2

GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.

  • CAS Number: 1312787-30-6
  • MF: C28H29NO6S2
  • MW: 539.66300
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FFA1 agonist-1

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].

  • CAS Number: 2417231-16-2
  • MF: C27H36ClNO3
  • MW: 458.03
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMG 837 hemicalcium salt

AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1, 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][2][3].

  • CAS Number: 1291087-14-3
  • MF: C26H21F3O3.1/2Ca
  • MW: 914.939
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TUG-424

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].

  • CAS Number: 1082058-99-8
  • MF: C18H16O2
  • MW: 264.318
  • Catalog: GPR40
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 448.1±38.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 205.9±21.4 °C

TAK-875

Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.

  • CAS Number: 1000413-72-8
  • MF: C29H32O7S
  • MW: 524.625
  • Catalog: GPR40
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 739.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 400.8±32.9 °C

DC 260126

DC260126, a small-molecule antagonist of GPR40.

  • CAS Number: 346692-04-4
  • MF: C16H18FNO2S
  • MW: 307.383
  • Catalog: GPR40
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 423.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 210.0±31.5 °C

Fasiglifam(TAK-875)

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[1][2][3][4].

  • CAS Number: 1374598-80-7
  • MF: C29H33O7.5S
  • MW: 533.63
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMG 837 (calcium hydrate)

AMG 837 calcium hydrate is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.IC50 value: 13 nM (EC50) [1]Target: GPR40 agonistAMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showedno significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potentand selective in vitro.

  • CAS Number: 1259389-38-2
  • MF: C26H22F3O4-
  • MW: 455.45
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SCO-267

SCO-267 is an allosteric GPR40 full agonist. SCO-267 can be used for the research of chronic diseases including diabetes[1].

  • CAS Number: 1656261-09-4
  • MF: C36H46N4O5
  • MW: 614.77
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GPR40 agonist 1

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.

  • CAS Number: 1853982-41-8
  • MF: C27H30FN3O4
  • MW: 479.54
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AM-1638

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

  • CAS Number: 1142214-62-7
  • MF: C33H35FO4
  • MW: 514.62700
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A