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名称

PF-02413873

英文别名

英文名称

PF-02413873

货号

P648420-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

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 In Vitro PF-02413873 shows potent PR antagonist activity with a derived K i 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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: t 1/2 =4.2 h, C max =162 ng/mL, CL/F=41 mL/min/kg. Form:Solid IC50& Target:Ki: 2.6 nM (progesterone receptor)

生化机理

PF-02413873（PF-2413873）是一种强效选择性、完全竞争性和口服活性的非甾体孕酮受体（PR）拮抗剂，其 K i 为 2.6 nM。PF-02413873 可阻断孕酮的结合和 PR 的核转位，并抑制子宫内膜的生长。

CAS号

936345-35-6

分子式

C18H21N3O3S

分子量

359.44 g/mol

PubChem编号

16662425

Isomeric SMILES

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

IIUPAC Name

4-[3-cyclopropyl-5-methyl-1-(methylsulfonylmethyl)pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile

INCHI

1S/C18H21N3O3S/c1-11-7-15(8-12(2)16(11)9-19)24-18-13(3)21(10-25(4,22)23)20-17(18)14-5-6-14/h7-8,14H,5-6,10H2,1-4H3

InChi Key

QSFGZNVRVZHUGV-UHFFFAOYSA-N

Smiles

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

PubChem CID

16662425

溶解性

DMSO : 100 mg/mL (278.21 mM; ultrasonic and warming and heat to 60°C)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

359.13 Da

单同位素质量Monoisotopic Mass

359.13 Da

拓扑极表面积Topological Polar Surface Area

93.400 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

622.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

2.600

RIDADR

NONHforallmodesoftransport

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

user reviews

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