Fasiglifam (TAK-875)

Catalog No.S2637

Fasiglifam (TAK-875) Chemical Structure

Molecular Weight(MW): 533.63

Fasiglifam (TAK-875) is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.

Size Price Stock Quantity  
In DMSO USD 580 In stock
USD 270 In stock
USD 370 In stock
USD 970 In stock
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2 Customer Reviews

  • INS-1 cells were incubated with 50 uM palmitate or BSA in the presence or absence of 5 uM TAK 875 for 30 min, followed by stimulation with 16.6 mm [U-13C]glucose for 30 min. Under these conditions, the following were measured: fructose bisphosphate (FBP) (I), NADH/NAD+ ratio (J). Error bars represent mean ?S.E. n = 3-4.

    J Biol Chem 2014 289(19), 13575-88. Fasiglifam (TAK-875) purchased from Selleck.

    The selective GPR40 agonist, TAK- 875, also has a selective inhibitory effect on the growth of all three human melanoma cell lines tested without negatively effecting the growth of the control fibroblast or human breast cancer cell lines even at very high concentrations.

    J Surg Res 2014 188(2):451-8. Fasiglifam (TAK-875) purchased from Selleck.

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Biological Activity

Description Fasiglifam (TAK-875) is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.
Features More potent at activating hGPR40 than oleic acid.
Targets
GPR40 [1]
(CHO cells expressing human GPR40)
14 nM(EC50)
In vitro

TAK-875 exhibits potent agonist activity and high binding affinity to the human GPR40 receptor with Ki of 38 nM. TAK-875 displays weaker affinity toward the rat GPR40 receptor with Ki of 140 nM. TAK-875 displays excellent selectivity, as TAK-875 has little agonist potency to other members of the FFA receptor family with EC50 of >10 μM. [1] TAK-875 treatment induces a concentration-dependent increase in intracellular IP production in CHO-hGPR40 with EC50 of 72 nM, more potently than that of endogenous ligand agonist oleic acid which requires much higher ligand concentrations to activate the receptor with EC50 of 29.9 μM. Neither TAK-875 nor oleic acid elicits an IP response in control CHO cells devoid of hGPR40. Consistent with the activation of the Gqα-mediated signaling pathway, TAK-875 augments glucose-dependent insulin secretion in pancreatic β cells. Prolonged stimulation of GPR40/FFA1 by TAK-875 does not cause pancreatic β Cell dysfunction or induction of apoptosis. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human 1321N1 cells MkXHSpVv[3Srb36gZZN{[Xl? MmW2RYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGSmEyKHKnY3XweI9zKGW6cILld5Nm\CCrbjDoeY1idiBzM{KxUlEh[2WubIOgZZN{\XO|ZXSgZZMh[2GuY3n1cUBud2KrbHn6ZZRqd25iYomg[ox2d3Knc3PlcoNmKHOyZXP0do9xcG:2b33leJJ6NCCHQ{WwQVE1NjF|IH7N NE\pSoEzOTh3NEC3OC=>
CHO cells NYPGcpBVTnWwY4Tpc44h[XO|YYm= MXLB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFfQOFAhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFPIU{Bk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCrboTyZYNmdGy3bHHyJINidGOrdX2gcIV3\WxiZn;yJFkxKHOnY4OgZpkhTkyLUGKgZZN{[XliaX6geIhmKHC{ZYPlcoNmKG:oIECuNUUhSlODLDDFR|UxRTBwMEG2JO69VQ>? M{XWfVIzPDlyME[3

... Click to View More Cell Line Experimental Data

In vivo In a rat model of diabetes, single oral dosing of TAK-875 at 0.3-3 mg/kg reduces the blood glucose excursion and augments insulin secretion during an oral glucose tolerance test, when TAK-875 is administered 1 hour before an oral glucose challenge. [1] In type 2 diabetic N-STZ-1.5 rats, administration of TAK-875 (1-10 mg/kg p.o.) shows a clear improvement in glucose tolerance and augments insulin secretion. Additionally, TAK-875 (10 mg/kg, p.o.) significantly augments plasma insulin levels and reduces fasting hyperglycemia in male Zucker diabetic fatty rats, whereas in fasted normal Sprague-Dawley rats, TAK-875 neither enhances insulin secretion nor causes hypoglycemia even at 30 mg/kg. [2]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Female Wistar fatty rats subjected to oral glucose tolerance test
  • Formulation: Formulated in 0.5% methylcellulose
  • Dosages: ~3 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (187.39 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
0.5% CMC+0.25% Tween 80
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 533.63
Formula

C29H32O7S.1/2H2O

CAS No. 1374598-80-7
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01834274 Terminated Diabetes Mellitus, Type 2 Takeda June 2013 Phase 3
NCT01829464 Terminated Diabetes Takeda May 2013 Phase 3
NCT01829477 Terminated Diabetes Mellitus, Type 2 Takeda April 2013 Phase 3
NCT01647542 Terminated Type 2 Diabetes Mellitus Takeda October 2012 Phase 3
NCT01609582 Terminated Type 2 Diabetes|Cardiovascular Disease Takeda June 2012 Phase 3
NCT01585792 Completed Diabetic Patients Takeda May 2012 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID