PF-4693627|cas:1312815-93-2|西域试剂

PF-4693627

产品编号：Bellancom-125415| CAS NO：1312815-93-2| 分子式：C₂₆H₂₉Cl₂N₃O₃| 分子量：502.43

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-125415		￥8200.00	杭州北京（现货）

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PF-4693627

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 bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC₅₀=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).

体外研究

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

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

体内研究

PF-4693627 (10 mg/kg; orally) inhibits 63% of PGE2 production relative to vehicle control in Guinea pig carrageenan stimulated air pouch model.
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.

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

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

Animal Model:	Sprague-Dawley rats.
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.

体内研究

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

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

Animal Model:	Sprague-Dawley rats.
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.

性状

Solid

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式