PF-02413873 是一种非甾体孕酮受体的竞争性拮抗剂,Ki 为 2.6 nM。 PF-02413873 可用于治疗子宫内膜异位症等妇科疾病的研究。
产品描述
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.
体外活性
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].
体内活性
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].
Cas No.
936345-35-6
分子式
C18H21N3O3S
分子量
359.44
别名
PF02413873
储存和溶解度
DMSO:95 mg/mL (264.30 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years