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CAS No.: 1640292-55-2

奥拉替尼马来酸盐 Catalog No. CSN19239

Synonyms: PF-03394197 maleate;PF-03394197;PF-03394197 Fumarate

Oclacitinib Fumarate is a potent JAK inhibitor with IC50 value ranging in 10-99 nM for JAK family members, most potent against JAK1 with IC50 value of 10 nM.

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技术信息

生物活性

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2050 mL
- 11.0251 mL
- 22.0501 mL
- 5 mM
- 0.4410 mL
- 2.2050 mL
- 4.4100 mL
- 10 mM
- 0.2205 mL
- 1.1025 mL
- 2.2050 mL

技术信息

CAS号

1640292-55-2

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H27N5O6S

运输

蓝冰

分子量

453.51

别名

PF-03394197 maleate;PF-03394197;PF-03394197 Fumarate;奥拉替尼马来酸盐

溶解度

DMSO	210.0 mg/mL (463.1 mM) warming
Water	120.0 mg/mL (264.6 mM) warming

动物实验配方

0.5% CMC-Na

30 mg/mL

suspension

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