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  3. PF-02413873

PF-02413873 (Synonyms: PF-2413873)

目录号: HY-11028
产品使用指南

PF-02413873 (PF-2413873) 是一种有效的、选择性、完全竞争性和口服活性的非甾体孕酮受体 (PR) 拮抗剂,Ki 值为 2.6 nM。PF-02413873 可以阻断孕激素结合和 PR 核易位,并在体内抑制子宫内膜的生长。

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PF-02413873 Chemical Structure

PF-02413873 Chemical Structure

CAS No. : 936345-35-6

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Description

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[1][2].

IC50 & Target

Ki: 2.6 nM (progesterone receptor)[1]

In Vitro

PF-02413873 shows potent PR antagonist activity with a derived Ki of 9.7 nM in the T47D native functional assay[1].
PF-02413873 (1 nM-10 μM) induces nuclear translocation only at high concentrations (>3 μM)[1].

In Vivo

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[1].
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)[1].

Animal Model: Cynomolgus macaques (3.7-5.7 kg; 5-6 years)[1]
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)[1]
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.
Molecular Weight

359.44

Formula

C₁₈H₂₁N₃O₃S

CAS No.

936345-35-6

SMILES

N#CC1=C(C)C=C(OC2=C(C)N(CS(=O)(C)=O)N=C2C3CC3)C=C1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PF-02413873PF-2413873PF02413873PF 02413873PF2413873PF 2413873Progesterone ReceptorNR3C3nonsteroidalprogesteronePRnucleartranslocationendometrialInhibitorinhibitorinhibit

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HY-11028
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