您的位置：首页 > 产品中心 > 603108-44-7， Glucokinase Activator, Cpd A-CAS 603108-44-7-Calbiochem
Glucokinase Activator, Cpd A-CAS 603108-44-7-Calbiochem
| 产品编号： | 4083849 |
| 规格： | The Glucokinase Activator, Cpd A, also referenced under CAS 603108-44-7, modulates Glucokinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications. |
| CAS NO： | 603108-44-7 |
| 包装规格： | 5 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
603108-44-7
Glucokinase Activator, Cpd A-CAS 603108-44-7-Calbiochem
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
基本信息
| Empirical Formula【经验(实验)分子式】 | C14H14N6OS2 |
| Molecular weight | 346.43 |
| General description【一般描述】 | 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. |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
| Other Notes【其他说明】 | 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. Structure12, 429. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥95% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | off-white |
| solubility【溶解性】 | DMSO: 5 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | 5 mg in Plastic ampoule Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 1 |
