PF-02413873

UNII-FH83GLG04S | Q27277988 | 4-[3-cyclopropyl-5-methyl-1-(methylsulfonylmethyl)pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile | 4-((3-cyclopropyl-5-methyl-1-((methylsulfonyl)methyl)-1H-pyrazol-4-yl)oxy)-2,6-dimethylbenzonitrile | PF-02413873, >=98% (HPLC) | H

PF-02413873

P648420-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

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)

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。

936345-35-6

C18H21N3O3S

359.44 g/mol

16662425

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

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

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

QSFGZNVRVZHUGV-UHFFFAOYSA-N

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

16662425

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

0

5

5

359.13 Da

359.13 Da

93.400 Ų

25

0

622.000

0

1

2.600

NONHforallmodesoftransport