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.
Cited by 5 Publications
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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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Choose Selective GPR Inhibitors
|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.|
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.  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. 
|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.  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. |
|In vitro||DMSO||100 mg/mL (187.39 mM)|
|In vivo||Add solvents individually and in order:
0.5% CMC+0.25% Tween 80
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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|
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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