TAK-875 Inhibitor CAS No. 1374598-80-7

Cat. No.	Name	Size	Price
KI1403	TAK-875	5 mg	$432
	TAK-875	10 mg	$592
	TAK-875	50 mg	$1552
	TAK-875	200 mg	$4272

Chemical Characteristic

Product Name	TAK-875
CAS No.	1374598-80-7
Molecular Weight	533.63
Formula	C₂₉H₃₂O₇S.₁/₂H₂O
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
Smiles	O1C[C@H](c2c1cc(cc2)OCc1cc(ccc1)c1c(cc(cc1C)OCCCS(=O)(=O)C)C)CC(=O)O
Chemical Structure

Biological activities

TAK-875 is a selective and orally bioavailable GPR40/ FFA_{1 agonist with an EC_{50 of 14 nM. TAK-875 exhibits high binding affinity with K_{ι of 38 nM to the human GPR40. ^[1] In addition, TAK-875 enhances glucose-dependent insulin secretion in a manner consistent with activation of the Gqα-mediated pathway. ^[2] TAK-875 exhibits rapid absorption, high C_{max, and high plasma exposure with high bioavailabilities in rats and dogs. ^[1] TAK-875 (0.1-10 µM) dose-dependently augments intracellular IP production in rat insulinoma INS-1 833/15 cells. TAK-875 augments insulin secretion and improves glucose tolerance during the oral glucose tolerance test in type 2 diabetic rats. Single oral administration of TAK-875 (1-10 mg/kg) to rats 1 hour before an oral glucose load results in a potent and dose-dependent reduction of glucose excursion.^[2]}}}}

Protocols

In vitro: TAK-875 is dissolved in DMSO. ^[1]

References

[1] Negoro N, et al. Discovery of TAK-875: a Potent, selective, and orally bioavailable GPR40 agonist. ACS Med.Chem.Lett. 2010, 1 (6): 290-294. [2] Tsujihata Y, 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.

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