PF-4693627
目录号: PL09523
CAS No. :1312815-93-2
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中文名称
PF-4693627
英文名称
PF-4693627
英文别名
PF-4693627
Cas No.
1312815-93-2
分子式
C26H29N3O3Cl2
分子量
502.43
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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 (IC 50 =3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
性状
Solid
IC50 & Target[1][2]
IC50: 3 nM (mPGES-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.
PF-4693627 shows high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC50=109 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
参考文献
[1]. Arhancet GB, et al. Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1114-9.
溶解度数据
In Vitro: DMSO : 100 mg/mL (199.03 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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