PF-02413873

PF-02413873CAS号: 936345-35-6分子式: C18H21N3O3S分子量: 359.44描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
PF-02413873 is a competitive antagonist of nonsteroidal progesterone receptor with a Ki of 2.6 nM. PF-02413873 can be used in studies about the treatment of gynecological conditions such as endometriosis.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:95 mg/mL (264.30 mM)
生物活性
靶点
Progesterone receptor:2.6 nM (Ki)
In vitro(体外研究)
PF-02413873 induces nuclear translocation only at high concentrations (>3 μM). PF-02413873 shows a derived Ki of 9.7 nM in the T47D native functional assay[3].
In vivo(体内研究)
In cynomolgus macaques, PF-02413873 (3 mg/kg; p.o.) exhibits a t1/2 of 4.2 h, a Cmax of 162 ng/mL and CL/F of 41 mL/min/kg. PF-02413873 (2.5 and 10 mg/kg; p.o.) reduces the endometrial thickness of 43 and 56%, respectively[3].