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MB05032

更新时间:2024-07-15 12:34:16 采购访问:7次

常用名 MB05032 CAS号 261365-11-1
价格 纯度 99.0%
备货期 10天 库存 现货
 产品详情(用途,包装等)
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

上海念兴实业有限公司 认证供应商

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参考价格:$264/10mM*1mLinDMSO
其他供应商价格:
2022-03-04 MB05032
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2024-07-15 MB05032
价格:需询单
2021-02-06 MB05032
价格:¥1669.0

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