PF-02413873|936345-35-6|(PF-2413873)-陌孚医药/Medlife

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PF-02413873 (Synonyms: PF-2413873)

目录号: PL10076 纯度: ≥99%

CAS No. :936345-35-6

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中文名称	PF-02413873
英文名称	PF-02413873
英文别名	Benzonitrile, 4-[[3-cyclopropyl-5-methyl-1-[(methylsulfonyl)methyl]-1H-pyrazol-4-yl]oxy]-2,6-dimethyl-;4-[3-cyclopropyl-5-methyl-1-(methylsulfonylmethyl)pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile;4-3-Cyclopropyl-5-methyl-1-(methylsulfonylmethyl)pyrazol-4-yloxy-2,6-dimethylbenzonitrile;PF-2413873;4-[3-Cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile;4-[[3-Cyclopropyl-5-methyl-1-[(methylsulfonyl)methyl]-1H-pyrazol-4-yl]oxy]-2,6-dimethyl-benzonitrile;PF 2413873;4-[[3-Cyclopropyl-5-methyl-1-[(methylsulfonyl)methyl]-1H-pyrazol-4-yl]oxy]-2,6-dimethylbenzonitrile (ACI);4-[3-Cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile;PF 02413873;PF-02413873
Cas No.	936345-35-6
分子式	C₁₈H₂₁N₃O₃S
分子量	359.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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，K_i 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。

生物活性

PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a K i of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo.

性状

Solid

IC50 & Target[1][2]

Ki: 2.6 nM (progesterone receptor)

体外研究(In Vitro)

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). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.
PF-02413873 (3 mg/kg; a single p.o.) exhibits t 1/2 (4.2 h), C max (162 ng/mL) and CL/F (41 mL/min/kg). has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Howe DC, et, al. The translational efficacy of a nonsteroidal progesterone receptor antagonist, 4-[3-cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on endometrial growth in macaque and human. J Pharmacol
[2]. Bungay PJ, et, al. Preclinical and clinical pharmacokinetics of PF-02413873, a nonsteroidal progesterone receptor antagonist. Drug Metab Dispos. 2011 Aug;39(8):1396-405.

溶解度数据	In Vitro: DMSO : 100 mg/mL (278.21 mM; ultrasonic and warming and heat to 60°C)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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