Oclacitinib maleate (PF-03394197 ) 一种新型 JAK 抑制剂-文献综述-资讯-生物在线

Oclacitinib maleate (PF-03394197 ) 一种新型 JAK 抑制剂

作者:MedChemExpress LLC 2019-12-31T00:00 (访问量:5542)

产品名: Oclacitinib maleate (别名: PF-03394197 maleate)

产品介绍:

Oclacitinib maleate (PF-03394197 maleate) 是一种新型 JAK 抑制剂。Oclacitinib maleate (PF-03394197 maleate) 抑制 JAK1 最有效,IC50 为 10 nM。

靶点作用:

JAK1

10 nM (IC50)
   

JAK2

18 nM (IC50)
   

Tyk2

84 nM (IC50)
   

JAK3

99 nM (IC50)

体内作用原理:

Scratching bouts at the high dose in the Oclacitinib group are significantly less than in the vehicle-only group (P<0.01)[2]. Client-owned dogs (n=436) with moderate to severe owner-assessed pruritus and a presumptive diagnosis of allergic dermatitis are enrolled. Dogs are randomized to either Oclacitinib at 0.4-0.6 mg/kg orally twice daily or an excipient-matched placebo. An enhanced 10 cm visual analog scale (VAS) is used to assess the severity of pruritus from day 0 to 7 and to assess the severity of dermatitis on days 0 and 7. Dogs can remain on the study for 28 days. Oclacitinib produces a rapid onset of efficacy within 24 h[3].

溶解参考方案:



请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。

参考文献:

 

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