merck millipore,默克密理博,346021,Glucokinase Activator, Cpd A - CAS 603108-44-7

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Merck Millipore 默克密理愽

merck millipore,默克密理博,346021,Glucokinase Activator, Cpd A - CAS 603108-44-7 - Calbiochem

经验配方	CAS号
C₁₄H₁₄N₆OS₂	603108-44-7

描述
概述	A cell-permeable thiazolylamide glucokinase (GK; Hexokinase IV/D) activator that reversibly targets a allosteric site that is only exposed for binding in the glucose-bound GK conformation, but not in the unbound "super-open" GK conformation or the GKRP- (GK Regulatory Protein) bound GK, and effectively stabilizes GK in an active conformation as well as prevents its interaction with and nuclear sequestration by GKRP, while exhibiting little effect against Hexokinase I/II/III. Compound A is shown to activate GK activity in cell-free assays (EC₅₀ = 0.42 and 0.14 µM in the presence of 2.5 mM and 10 mM of glucose, respectively) and effectively induce cellular GK activation and increase glucose metabolism both in in rats (10 to 30 mg/kg, p.o.) in vivo and in rat islets and hepatocytes cultures (10 to 30 µM) in vitro.
产品目录编号	346021
品牌系列	Calbiochem®
同义词	Hexokinase D Activator, Hexokinase IV Activator, 2-Amino-5-(4-methyl-4H-(1,2,4)-triazole-3-yl-sulfanyl)-N-(4-methyl-thiazole-2-yl)benzamide, Compound A

参考
参考	Iino, T., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5531. Mitsuya, M., et al. 2009. Bioorg. Med. Chem. Lett. 19, 2718. Nishimura, T., et al. 2009. Bioorg. Med. Chem. Lett. 19, In press. Futamura, M., et al. 2006. J. Biol. Chem. 281, 1357. Kamata, K., et al. 2004. Structure 12, 429.

生物信息
纯度	≥95% by HPLC

理化信息
溶解度	DMSO

安全信息
S相	S: 22-24/25-36 Do not breathe dust. Avoid contact with skin and eyes. Wear suitable protective clothing.

储存和货运信息
货运代码	Ambient Temperature Only
毒性	Standard Handling
储存	+2°C to +8°C
避光	Protect from light
无需冷冻	No
特殊指南	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

包装信息
惰性气体下包装	Packaged under inert gas

merck millipore,默克密理博,346021,Glucokinase Activator, Cpd A - CAS 603108-44-7 - Calbiochem

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