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Gamma Secretase

TAK875 (1374598-80-7)

TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid. TAK-875 is a novel, orally available, selective GPR40 agonist. TAK-875 exhibits potent agonist activity and high binding affinity to the human GPR40 receptor with Ki of 38 nM.

Not Intended for Therapeutic Use. For research use only.

CAS: 1374598-80-7 Category

TAK875 (1374598-80-7) Description:

TAK-875 is a novel, orally available, selective GPR40 agonist. TAK-875 exhibits potent agonist activity and high binding affinity to the human GPR40 receptor with Ki of 38 nM. TAK-875 enhanced glucose-induced insulin secretion in a glucose-dependent manner in both human and rat islets. In rat insulinoma INS-1 833/15 cells, TAK-875 increased intracellular inositol monophosphate and calcium concentration, consistent with activation of the Gqα signaling pathway. In addition, TAK-875 (10 mg/kg, p.o.) significantly augmented plasma insulin levels and reduced fasting hyperglycemia in male Zucker diabetic fatty rats, whereas in fasted normal Sprague-Dawley rats, TAK-875 neither enhanced insulin secretion nor caused hypoglycemia even at 30 mg/kg. TAK-875 improves both postprandial and fasting hyperglycemia with a low risk of hypoglycemia and no evidence of β cell toxicity. TAK-875 significantly improved glycaemic control in patients with type 2 diabetes with minimum risk of hypoglycaemia.

TAK875 (1374598-80-7) Specifications:

Product Name TAK875
Synonyms TAK875; TAK-875; TAK 875; Fasiglifam.
Chemical Names (S)-2-(6-((2′,6′-dimethyl-4′-(3-(methylsulfonyl)propoxy)-[1,1′-biphenyl]-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 1374598-80-7
Molecular Formula C58H66O15S2
Molecular Weight 1067.26564
Monoisotopic Mass 1066.384 g/mol
MDL number MFCD18251445
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
SMILES CS(=O)(=O)CCCOc1cc(C)c(-c2cc(COc3cc4OC[[email protected]@H](CC(O)=O)c4cc3)ccc2)c(C)c1
Form Powder
Color white to off-white
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly.
Handling Protect from air and light
Application TAK-875, is a potent, selective, and orally bioavailable GPR40 agonist, with a pharmacokinetic profile enabling long-acting drug efficacy.



RIDADR NONH for all modes of transport


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