产品
编 号:F396594
分子式:C18H23FN2O6
分子量:382.38
产品类型
结构图
CAS No: 582316-00-5
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产品详情
生物活性:
MX1013 is a potent, irreversible dipeptide caspase inhibitor vith?antiapoptotic activity. MX1013 inhibits recombinant human caspase 3 with an IC50?of 30 nM.
体内研究:
MX1013 is an effective antiapoptotic agent?in vivo. MX1013 not only inhibits local tissue apoptosis, but also can protect animals against its lethal effects.Animal Model:Female ND4 Swiss Webster mice (16.5-21 g)
Dosage:0, 0.25, 1, 10 mg/kg (formulated in an aqueous vehicle containing 50 mm?Tris-HCl, pH 8.0)
Administration:Injected i.v.
Result:The lowest dose of 0.25 mg/kg protected 66% of the mice from the lethal effects of anti-Fas antibody at the 3 h time point, and 1 and 10 mg/kg?dose protected 100% of the mice at the 3 h time point.
体外研究:
MX1013 inhibits caspases 1, 3, 6, 7, 8, and 9, with IC50?values ranging from 5 to 20 nm. MX1013 is selective for caspases, and is a poor inhibitor of noncaspase proteases, such as cathepsin B, calpain I, or Factor Xa (IC50?values >10?μm).MX1013 inhibits three key markers of apoptosis: the proteolytic maturation of caspase 3, the caspase-mediated cleavage of PARP, and the fragmentation of genomic DNA.