产品
编 号：F747419
分子式：C24H29ClN6O2
分子量：468.98
分子式：C24H29ClN6O2
分子量：468.98
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 1824708-03-3
产品详情
生物活性：
Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension.
体内研究：
Smurf1-IN-1 (Compound 38) (1，3，10 mg/kg，口服) 对大鼠肺部高压模型有显著疗效。Smurf1-IN-1 (静脉注射1 mg/kg，口服 3 mg/kg) 显示 T1/2 为 7.9 小时，口服生物利用度 (F%) 为 82%。 Pharmacokinetic parameters for Smurf1-IN-1 (Compound 38) in rats dose and route oral bioavailability (%) p.o. AUClast (nM ? h /mL)p.o. Cmax (nM/L)half-life (h) claearance (mL/min/kg) Vss (1/kg)
3 mpg p.o./1 mpg i.v.82738320077.917.12.3
Animal Model:Hypoxia-Sugen rat model of PAH
Dosage:1, 3, 10 mg/kg
Administration:Oral gavage (p.o.)
Result:Caused a 10% increase in muscularization at day 14 and progression to around 18% muscularization was observed in the vehicle group by the end of the study at a dose of 3 mg/kg.
Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension.
体内研究：
Smurf1-IN-1 (Compound 38) (1，3，10 mg/kg，口服) 对大鼠肺部高压模型有显著疗效。Smurf1-IN-1 (静脉注射1 mg/kg，口服 3 mg/kg) 显示 T1/2 为 7.9 小时，口服生物利用度 (F%) 为 82%。 Pharmacokinetic parameters for Smurf1-IN-1 (Compound 38) in rats dose and route oral bioavailability (%) p.o. AUClast (nM ? h /mL)p.o. Cmax (nM/L)half-life (h) claearance (mL/min/kg) Vss (1/kg)
3 mpg p.o./1 mpg i.v.82738320077.917.12.3
Animal Model:Hypoxia-Sugen rat model of PAH
Dosage:1, 3, 10 mg/kg
Administration:Oral gavage (p.o.)
Result:Caused a 10% increase in muscularization at day 14 and progression to around 18% muscularization was observed in the vehicle group by the end of the study at a dose of 3 mg/kg.
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