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Oclacitinib

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Chemical Structure| 1208319-26-9 同义名 : PF-03394197
CAS号 : 1208319-26-9
货号 : A124514
分子式 : C15H23N5O2S
纯度 : 98%+
分子量 : 337.44
MDL号 : MFCD25976611
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(133.36 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Using isolated enzyme systems and in vitro human or canine cell models, the efficacy and specificity of Oclacitinib are assessed against members of the JAK family and the cytokines that initiate JAK activation in cells. The compound inhibits JAK1, JAK2, JAK3, and TYK2 with 50% inhibitory concentrations (IC50's) of 10, 18, 99, and 84 nM, respectively. Oclacitinib demonstrates its highest potency against JAK1, with 1.8-fold greater selectivity for JAK1 over JAK2 and 9.9-fold greater selectivity over JAK3. It inhibits members of the JAK family at concentrations ranging from 10 to 99 nM and shows no inhibition against a set of 38 unrelated kinases (IC50's > 1000 nM). Additionally, Oclacitinib blocks the activity of JAK1-dependent cytokines critical for allergic responses and inflammation (IL-2, IL-4, IL-6, and IL-13) and pruritus (IL-31), with IC50 values between 36 and 249 nM. It has minimal impact on cytokines that do not activate the JAK1 enzyme (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC50's > 1000 nM) [1]. Topical application of Tofacitinib (0.1%) and Oclacitinib (0.1%) significantly decreases cell migration from mouse ear explants compared to vehicle-treated ears (all P < 0.05). Additionally, the number of MHC class II positive cells (Langerhans cells) is substantially reduced in epidermis treated with vehicle compared to those treated with each JAK inhibitor (all P < 0.01) [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.82mL

2.96mL

1.48mL

29.63mL

5.93mL

2.96mL
参考文献

[1]Gonzales AJ, et al. Oclacitinib (APOQUEL) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J Vet Pharmacol Ther. 2014 Aug;37(4):317-24.

[2]Fukuyama T, et al. Topically Administered Janus-Kinase Inhibitors Tofacitinib and Oclacitinib Display Impressive Antipruritic and Anti-Inflammatory Responses in a Model of Allergic Dermatitis. J Pharmacol Exp Ther. 2015 Sep;354(3):394-405.

[3]Cosgrove SB, et al. Efficacy and safety of oclacitinib for the control of pruritus and associated skin lesions in dogs with canine allergic dermatitis. Vet Dermatol. 2013 Oct;24(5):479-e114.