MB05032

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更新时间： 2025-08-26 18:00:08

CAS号：261365-11-1

常用名： MB05032

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纯度： 99.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： MB05032 is a special and efficacious GNG inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM. IC50 Value: 16 nM (Human Liver FBPase) [1]Target: Fructose 1, 6-bisphosphataseOral delivery of MB05032 was achieved by using the bisamidate prodrug MB06322 (CS-917), which is converted to MB05032 in two steps through the action of an esterase and a phosphoramidase.in vitro: MB05032 inhibits human liver FBPase with a potency (IC50 = 16 ± 1.5 nM) significantly greater than the natural inhibitor, AMP (IC50 = 1 μM), and the most well characterized AMP mimetic, ZMP (IC50 = 12 ± 1.4 μM). MB05032 inhibits rat FBPase 3-fold weaker (IC50 of 61 ± 4 nM) than human FBPase, whereas AMP is 20-fold weaker as an inhibitor [1]. Inhibition of FBPase activity in islet β-cells by its specific inhibitor MB05032 led to significant increase of their glucose utilization and cellular ATP to ADP ratios and consequently enhanced GSIS in vitro [2]. in vivo: Oral administration of MB06322 to young (8-9 weeks old) ZDF rats with mild diabetes (basal insulin levels of 7.7 ± 0.7 ng/ml) and aged (12-13 weeks) ZDF rats with overt diabetes (basal insulin levels of 0.65 ± 0.16 ng/ml) results in dose-dependent glucose lowering. The dose-response is relatively steep, with 6-10 mg/kg and 30-100 mg/kg being the approximate doses associated with minimal and maximal activity, respectively [1]. Pretreatment of mice with the MB05032 prodrug MB06322 could potentiate GSIS in vivo and improve their glucose tolerance [2].Toxicity: Neither lactate nor triglycerides increased in 8- to 9-week-old ZDF rats with mild diabetes treated with high doses of MB06322. In ZDF rats with more advanced disease, lactate and triglyceride levels were elevated but only modestly ( 物理化学性质： CAS号：261365-11-1 常用中文名：MB05032 常用英文名：MB05032 分子式：C11H15N2O4PS 分子量：302.28700 密度：N/A 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：2-8℃

供应商信息：

公司名：上海化源世纪贸易有限公司推荐

认证状态： 已认证供应商

商品数： 396716件

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其他供应商价格：

2022-03-04 价格：￥2969.9 MB05032

2021-02-06 价格：￥1669.0 MB05032

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MB05032价格

MB05032

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