产品
编 号：F527739
分子式：C18H21N3O3S
分子量：359.44
分子式：C18H21N3O3S
分子量：359.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 936345-35-6
产品详情
生物活性：
PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo.
体内研究：
PF-02413873 (2.5 and 10 mg/kg; p.o. twice daily for 10 days) induces a statistically significant reduction in endometrial thickness in cynomolgus macaques.PF-02413873 (3 mg/kg; a single p.o.) exhibits t1/2 (4.2 h), Cmax (162 ng/mL) and CL/F (41 mL/min/kg).Animal Model:Cynomolgus macaques (3.7-5.7 kg; 5-6 years)
Dosage:2.5, 10 mg/kg
Administration:P.o. twice daily for 10 days
Result:Reduced the endometrial thickness of 43 and 56% at the dose of 2.5 and 10 mg/kg, respectively.
Animal Model:Cynomolgus macaques (3.7-5.7 kg; 5-6 years)
Dosage:3 mg/kg (Pharmacokinetic Analysis)
Administration:A single p.o.
Result:t1/2=4.2 h, Cmax=162 ng/mL, CL/F=41 mL/min/kg.
体外研究：
PF-02413873 shows potent PR antagonist activity with a derived Ki of 9.7 nM in the T47D native functional assay.PF-02413873 (1 nM-10 μM) induces nuclear translocation only at high concentrations (>3 μM).
PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo.
体内研究：
PF-02413873 (2.5 and 10 mg/kg; p.o. twice daily for 10 days) induces a statistically significant reduction in endometrial thickness in cynomolgus macaques.PF-02413873 (3 mg/kg; a single p.o.) exhibits t1/2 (4.2 h), Cmax (162 ng/mL) and CL/F (41 mL/min/kg).Animal Model:Cynomolgus macaques (3.7-5.7 kg; 5-6 years)
Dosage:2.5, 10 mg/kg
Administration:P.o. twice daily for 10 days
Result:Reduced the endometrial thickness of 43 and 56% at the dose of 2.5 and 10 mg/kg, respectively.
Animal Model:Cynomolgus macaques (3.7-5.7 kg; 5-6 years)
Dosage:3 mg/kg (Pharmacokinetic Analysis)
Administration:A single p.o.
Result:t1/2=4.2 h, Cmax=162 ng/mL, CL/F=41 mL/min/kg.
体外研究：
PF-02413873 shows potent PR antagonist activity with a derived Ki of 9.7 nM in the T47D native functional assay.PF-02413873 (1 nM-10 μM) induces nuclear translocation only at high concentrations (>3 μM).
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