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Oclacitinib maleate

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Chemical Structure| 1640292-55-2 同义名 : PF-03394197 maleate;PF-03394197;Oclacitinib maleate
CAS号 : 1640292-55-2
货号 : A265661
分子式 : C19H27N5O6S
纯度 : 98+%
分子量 : 453.51
MDL号 : MFCD30533388
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(551.25 mM)，配合低频超声助溶，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

H2O: 5 mg/mL(11.03 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • JAK1

    JAK1, IC50:10nM

  • JAK3

    JAK3, IC50:99nM

  • Tyk2

    TYK2, IC50:84nM

  • JAK2

    JAK2, IC50:18nM
描述 Janus kinase (JAK) enzymes are a family of tyrosine kinases consisting of four members: JAK1, JAK2, JAK3, and TYK2. Oclacitinib is a potent JAK1 inhibitor with an IC50 value of 10nM. It also inhibits JAK2, JAK3, and TYK2 with IC50 values of 18, 99, and 84nM, respectively. Oclacitinib inhibited the function of JAK1-dependent cytokines involved in allergy, inflammation, and pruritus, including interleukin (IL)-2, IL-4, IL-6, IL-13, and IL-31 with IC50 values ranging from 36 to 249nM[3]. In a mouse model of toluene-2,4-diisocyanate (TDI)-induced allergic dermatitis, topical administration of Oclacitinib (0.1%, 0.25%, and 0.5%) 30 minutes before and 4 h after TDI challenge resulted in a significant decrease in scratching behavior and ear thickness, as well as a reduction in the levels of inflammatory cytokines in the ear skin compared with the vehicle-treated group[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.03mL

2.21mL

1.10mL

22.05mL

4.41mL

2.21mL
参考文献

[1]Gonzales AJ, Bowman JW, 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]Collard WT, Hummel BD, et al. The pharmacokinetics of oclacitinib maleate, a Janus kinase inhibitor, in the dog. J Vet Pharmacol Ther. 2014 Jun;37(3):279-85.

[3]Gonzales AJ, Bowman JW, Fici GJ, Zhang M, Mann DW, Mitton-Fry M. Oclacitinib (APOQUEL(®)) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J Vet Pharmacol Ther. 2014;37(4):317-324. doi:10.1111/jvp.12101

[4]Fukuyama T, Ehling S, Cook E, Bäumer W. 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;354(3):394-405. doi:10.1124/jpet.115.223784