產品名： Oclacitinib maleate (別名: PF-03394197 maleate)

產品介紹：

Oclacitinib maleate (PF-03394197 maleate) 是一種新型 JAK 抑制劑。Oclacitinib maleate (PF-03394197 maleate) 抑制 JAK1 最有效，IC50 為 10 nM。

靶點作用：

JAK1

10 nM (IC50)
???

JAK2

18 nM (IC50)
???

Tyk2

84 nM (IC50)
???

JAK3

99 nM (IC50)

體內作用原理：

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].

溶解參考方案：

請根據您的實驗動物和給藥方式選擇適當的溶解方案。以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶

??? 1.

??? 請依序添加每種溶劑： 10% DMSO??? 40% PEG300??? 5% Tween-80??? 45% saline

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

??? 2.

??? 請依序添加每種溶劑： 10% DMSO??? 90% (20% SBE-β-CD in saline)

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

??? 3.

??? 請依序添加每種溶劑： 10% DMSO??? 90% corn oil

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

*以上所有助溶劑都可在 MCE 網站選購。

參考文獻：

?