Cofttek holdings limited

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
InChIKey BZCALJIHZVNMGJ-HSZRJFAPSA-N
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

References:

  • 1: Sylvain V, Lafarge S, Bignon YJ. Molecular pathways involved in response to ionizing radiation of ID-8 mouse ovarian cancer cells expressing exogenous full-length Brca1 or truncated Brca1 mutant. Int J Oncol. 2001 Sep;19(3):599-607. PubMed PMID: 11494042.
  • 2: Hasegawa K, Yasuda SY, Teo JL, Nguyen C, McMillan M, Hsieh CL, Suemori H, Nakatsuji N, Yamamoto M, Miyabayashi T, Lutzko C, Pera MF, Kahn M. Wnt signaling orchestration with a small molecule DYRK inhibitor provides long-term xeno-free human pluripotent cell expansion. Stem Cells Transl Med. 2012 Jan;1(1):18-28. doi: 10.5966/sctm.2011-0033. PubMed PMID: 23197636; PubMed Central PMCID: PMC3727690.
  • 3: Su F, Kozak KR, Imaizumi S, Gao F, Amneus MW, Grijalva V, Ng C, Wagner A, Hough G, Farias-Eisner G, Anantharamaiah GM, Van Lenten BJ, Navab M, Fogelman AM, Reddy ST, Farias-Eisner R. Apolipoprotein A-I (apoA-I) and apoA-I mimetic peptides inhibit tumor development in a mouse model of ovarian cancer. Proc Natl Acad Sci U S A. 2010 Nov 16;107(46):19997-20002. doi: 10.1073/pnas.1009010107. PubMed PMID: 21041624; PubMed Central PMCID: PMC2993420.
  • 4: Uchiyama A, Chang C, Suzuki S, Mashimo T, Fujino Y. An expiratory assist during spontaneous breathing can compensate for endotracheal tube resistance. Anesth Analg. 2009 Aug;109(2):434-40. doi: 10.1213/ane.0b013e3181aa5cdb. PubMed PMID: 19608814.
  • 5: Sylvain V, Lafarge S, Bignon YJ. Dominant-negative activity of a Brca1 truncation mutant: effects on proliferation, tumorigenicity in vivo, and chemosensitivity in a mouse ovarian cancer cell line. Int J Oncol. 2002 Apr;20(4):845-53. PubMed PMID: 11894135.