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TAK-875 | GPR40 agonist

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Catalog #:

Product Description

TAK-875 is an orally-available, benzofuran-based, agonist of GPR40 for the potential treament of Type 2 diabetes mellitus, with an human EC50 of 0.014 uM in a FLIPR assay. It has high selectivity over GPR41, GPR43, and GPR120, with EC50s all greater than 10 uM. [1] Oral dosing (0.3-3 mg/kg) of TAK-875 in a glucose intolerance test in female Wistar rats reduced blood glucose excursion. Insulin secretion was increased during an oral glucose tolerance test.

TAK-875 was shown to activate the Gqa-mediated signalling pathway in pancreatic b-cells. Prolonged agonist stimulation by TAK-875 revealed no evidence of b-cell dysfunction or toxicity, nor does it cause a induction of a marker of apoptosis in pancreatic b-cells. [2]

Technical information:

Chemical Formula:   C29H32O7S.1/2H2O
CAS #:   1000413-72-8
Molecular Weight:   533.63
Purity:   >98%
Appearance:   White
Chemical Name:   [(3S)-6-({2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy]biphe-nyl-3-yl}meth-oxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid hemi-hydrate
Solubility:   Up to 100mM in DMSO
Synonyms:   TAK-875, TAK875

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


1. Negoro et al., ACS Med. Chem. Lett. 2010, 1, 290-294.
2. Tsujihata et al., 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, 339(1), 228-237. Pubmed ID: 21752941

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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