PF-4693627

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PF-4693627

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1312815-93-2
包装:	10mg
市场价:	8200元

产品介绍

PF-4693627 是一种有效的，口服生物可利用的，选择性的微粒体前列腺素E合酶 (mPGES-1) 抑制剂 (IC₅₀=3 nM)，可用于骨关节炎和类风湿关节炎等的研究。

生物活性

PF-4693627 is a potent, selective and orally bioavailablemicrosomalprostaglandin E synthase-1 (mPGES-1) inhibitor (IC₅₀=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA)^[1].

IC₅₀& Target

IC50: 3 nM (mPGES-1)^[1]

体外研究
(In Vitro)

PF-4693627 also inhibits mPGES-1 with IC₅₀s of 180 and 6 nM in HWB-1483 and human fetal fibroblast, respectively^[1].
PF-4693627 shows high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC₅₀=109 nM)^[1].

体内研究
(In Vivo)

PF-4693627 (10 mg/kg; orally) inhibits 63% of PGE2 production relative to vehicle control in Guinea pig carrageenan stimulated air pouch model^[1].
PF-4693627 (1.0 mg/kg; i.v.) shows good bioavailability (59%) and modest half life (t_1/2=3.7 h) in Sprague-Dawley rats^[1].

Animal Model:	Guinea pig with carrageenan stimulated air pouch inflammation model^[1]
Dosage:	10 mg/kg
Administration:	Administered orally
Result:	63% PGE2 inhibition.

Animal Model:	Sprague-Dawley rats^[1].
Dosage:	1.0 mg/kg (Pharmacokinetic Analysis)
Administration:	Administered i.v.
Result:	Clearance (CL), volume of distribution (Vd_ss), t_1/2, mean residence time (MRT) and bioavailability (F) is 12 mL/min/kg, 3.0 L/kg, 3.7 h, 4.42 h, 59%, respectively.

分子量

502.43

性状

Solid

Formula

C₂₆H₂₉Cl₂N₃O₃

CAS 号

1312815-93-2

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
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL(199.03 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.9903 mL	9.9516 mL	19.9033 mL
5 mM	0.3981 mL	1.9903 mL	3.9807 mL
10 mM	0.1990 mL	0.9952 mL	1.9903 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。