WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 504110

CAS#: 1000413-72-8

Description: Fasiglifam, also known as TAK-875, is a potent, selective, and orally bioavailable GPR40 agonist, with a pharmacokinetic profile enabling long-acting drug efficacy. TAK-875 showed potent plasma glucose-lowering action and insulinotropic action during an oral glucose tolerance test in female Wistar fatty rats with impaired glucose tolerance. TAK-875 is currently in clinical trials for the treatment of type 2 diabetes mellitus.

Price and Availability


USD 90
USD 450
USD 2750

USD 150
USD 750
USD 4250

USD 250
USD 1750
USD 7450

Fasiglifam (TAK-875), purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 200mg may be 2 weeks.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 504110
Name: Fasiglifam
CAS#: 1000413-72-8
Chemical Formula: C29H32O7S
Exact Mass: 524.18687
Molecular Weight: 524.63
Elemental Analysis: C, 66.39; H, 6.15; O, 21.35; S, 6.11

Synonym: TAK875; TAK-875; TAK 875; Fasiglifam.

IUPAC/Chemical Name: (S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)-[1,1'-biphenyl]-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid


InChi Code: InChI=1S/C29H32O7S/c1-19-12-25(34-10-5-11-37(3,32)33)13-20(2)29(19)22-7-4-6-21(14-22)17-35-24-8-9-26-23(15-28(30)31)18-36-27(26)16-24/h4,6-9,12-14,16,23H,5,10-11,15,17-18H2,1-3H3,(H,30,31)/t23-/m1/s1


Technical Data

white to off-white solid powder

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:

Additional Information



1: Yabuki C, Komatsu H, Tsujihata Y, Maeda R, Ito R, Matsuda-Nagasumi K, Sakuma K, Miyawaki K, Kikuchi N, Takeuchi K, Habata Y, Mori M. A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1. PLoS One. 2013 Oct 10;8(10):e76280. doi: 10.1371/journal.pone.0076280. eCollection 2013. PubMed PMID: 24130766; PubMed Central PMCID: PMC3794927.

2: Naik H, Lu J, Cao C, Pfister M, Vakilynejad M, Leifke E. Pharmacometric Approaches to Guide Dose Selection of the Novel GPR40 Agonist TAK-875 in Subjects With Type 2 Diabetes Mellitus. CPT Pharmacometrics Syst Pharmacol. 2013 Jan 9;2:e22. doi: 10.1038/psp.2012.23. PubMed PMID: 23887592; PubMed Central PMCID: PMC3600727.

3: Ito R, Tsujihata Y, Matsuda-Nagasumi K, Mori I, Negoro N, Takeuchi K. TAK-875, a GPR40/FFAR1 agonist, in combination with metformin prevents progression of diabetes and β-cell dysfunction in Zucker diabetic fatty rats. Br J Pharmacol. 2013 Oct;170(3):568-80. doi: 10.1111/bph.12297. PubMed PMID: 23848179; PubMed Central PMCID: PMC3791995.

4: Kaku K, Araki T, Yoshinaka R. Randomized, double-blind, dose-ranging study of TAK-875, a novel GPR40 agonist, in Japanese patients with inadequately controlled type 2 diabetes. Diabetes Care. 2013 Feb;36(2):245-50. doi: 10.2337/dc12-0872. Epub 2012 Oct 18. PubMed PMID: 23086138; PubMed Central PMCID: PMC3554318.

5: Leifke E, Naik H, Wu J, Viswanathan P, Demanno D, Kipnes M, Vakilynejad M. A multiple-ascending-dose study to evaluate safety, pharmacokinetics, and pharmacodynamics of a novel GPR40 agonist, TAK-875, in subjects with type 2 diabetes. Clin Pharmacol Ther. 2012 Jul;92(1):29-39. doi: 10.1038/clpt.2012.43. Epub 2012 Jun 6. PubMed PMID: 22669289.

6: Burant CF, Viswanathan P, Marcinak J, Cao C, Vakilynejad M, Xie B, Leifke E. TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet. 2012 Apr 14;379(9824):1403-11. doi: 10.1016/S0140-6736(11)61879-5. Epub 2012 Feb 27. PubMed PMID: 22374408.

7: Yashiro H, Tsujihata Y, Takeuchi K, Hazama M, Johnson PR, Rorsman P. The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets. J Pharmacol Exp Ther. 2012 Feb;340(2):483-9. doi: 10.1124/jpet.111.187708. Epub 2011 Nov 21. PubMed PMID: 22106100.

8: Araki T, Hirayama M, Hiroi S, Kaku K. GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes. Diabetes Obes Metab. 2012 Mar;14(3):271-8. doi: 10.1111/j.1463-1326.2011.01525.x. Epub 2011 Dec 22. PubMed PMID: 22051148.

9: Tsujihata Y, Ito R, Suzuki M, Harada A, Negoro N, Yasuma T, Momose Y, Takeuchi K. TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J Pharmacol Exp Ther. 2011 Oct;339(1):228-37. doi: 10.1124/jpet.111.183772. Epub 2011 Jul 13. PubMed PMID: 21752941.

10: Naik H, Vakilynejad M, Wu J, Viswanathan P, Dote N, Higuchi T, Leifke E. Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of the GPR40 agonist TAK-875: results from a double-blind, placebo-controlled single oral dose rising study in healthy volunteers. J Clin Pharmacol. 2012 Jul;52(7):1007-16. doi: 10.1177/0091270011409230. Epub 2011 May 24. PubMed PMID: 21610201.

11: Molecule of the Month. TAK-875. Drug News Perspect. 2010 Dec;23(10):667. doi: 10.1358/dnp.2010.23.10.1560199. PubMed PMID: 21180652.