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TAK-875
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TAK-875图片
CAS NO:1000413-72-8
规格:98%
分子量:524.64
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
GPR40 agonist
CAS:1000413-72-8
分子式:C29H32O7S
分子量:524.64
纯度:98%
存储:Store at -20°C

Background:

TAK-875 is a potent, selective, and oral GPR40 agonist. GPR40 is one of the G protein-coupled receptors predominantly expressed in pancreatic β-cells, mediating enhancement of glucose-stimulated insulin secretion by free fatty acids.


In vitro: TAK-875 exhibited potent agonist activity and high binding affinity to the human receptor. In addition, TAK-875 showed excellent agonist potency selectivity for GPR40 receptor over other members of the FFA receptor family (for which EC50>10 μM) [1].


In vivo: 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 [2].


Clinical trial: TAK-875 acts as a glucose-dependent insulinotropic agent with low hypoglycemic risk. Its P K is suitable for once-daily oral administration.


参考文献:
[1] Negoro N, Sasaki S, Mikami S, Ito M, Suzuki M, Tsujihata Y, Ito R, Harada A, Takeuchi K, Suzuki N, Miyazaki J, Santou T, Odani T, Kanzaki N, Funami M, Tanaka T1, Kogame A, Matsunaga S, Yasuma T, Momose Y.  Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist. ACS Med Chem Lett. 2010 Jun 18;1(6):290-4.
[2] 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.