PF-4693627
目录号 : KM10430 CAS No. : 1312815-93-2 纯度 : 98%

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。

规格 价格 是否有货 数量
10mg
In-stock

Other Forms of Rapamycin:

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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).

IC50&Target

IC50: 3 nM (mPGES-1)

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).

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 (t1/2=3.7 h) in Sprague-Dawley rats.

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 (Vdss), t1/2, mean residence time (MRT) and bioavailability (F) is 12 mL/min/kg, 3.0 L/kg, 3.7 h, 4.42 h, 59%, respectively.
分子式
C26H29N3O3Cl2
分子量
502.43
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
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动物实验计算换算器
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工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。