Fasiglifam (TAK-875)

Catalog No.S2637

For research use only.

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.

Fasiglifam (TAK-875) Chemical Structure

CAS No. 1374598-80-7

Selleck's Fasiglifam (TAK-875) has been cited by 13 publications

Purity & Quality Control

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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 MWnGeY5kfGmxbjDhd5NigQ>? MoO1RYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGSmEyKHKnY3XweI9zKGW6cILld5Nm\CCrbjDoeY1idiBzM{KxUlEh[2WubIOgZZN{\XO|ZXSgZZMh[2GuY3n1cUBud2KrbHn6ZZRqd25iYomg[ox2d3Knc3PlcoNmKHOyZXP0do9xcG:2b33leJJ6NCCHQ{WwQVE1NjF|IH7N MlfXNlE5PTRyN{S=
CHO cells MWHGeY5kfGmxbjDhd5NigQ>? MVHB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFfQOFAhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFPIU{Bk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCrboTyZYNmdGy3bHHyJINidGOrdX2gcIV3\WxiZn;yJFkxKHOnY4OgZpkhTkyLUGKgZZN{[XliaX6geIhmKHC{ZYPlcoNmKG:oIECuNUUhSlODLDDFR|UxRTBwMEG2JO69VQ>? NUL5OZZIOjJ2OUCwOlc>
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 (from reference)

Animal Research:[1]
  • Animal Models: Female Wistar fatty rats subjected to oral glucose tolerance test
  • Dosages: ~3 mg/kg
  • Administration: Orally

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% CMC+0.25% Tween 80
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 533.63
Formula

C29H32O7S.1/2H2O

CAS No. 1374598-80-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=CC(=C1C2=CC=CC(=C2)COC3=CC4=C(C=C3)C(CO4)CC(=O)O)C)OCCCS(=O)(=O)C.CC1=CC(=CC(=C1C2=CC=CC(=C2)COC3=CC4=C(C=C3)C(CO4)CC(=O)O)C)OCCCS(=O)(=O)C.O

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01496443 Completed Drug: TAK-875 and Glimepiride Pharmacokinetics Takeda January 2012 Phase 1
NCT00949091 Completed Drug: TAK-875 Diabetes Mellitus Type 2 Takeda January 2009 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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