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Oclacitinib-13C-d3 is intended for use as an internal standard for the quantification of oclacitinib (Item No. 18722) by GC- or LC-MS. Oclacitinib is an inhibitor of the JAK family kinases JAK1, JAK2, JAK3, and TYK2 (IC50s = 10, 18, 99, and 84 nM, respectively).1 It is selective for JAK kinases over a panel of 38 additional kinases at 1 μM. Oclacitinib inhibits LPS-induced increases in IL-12 and TNF-α levels in murine bone marrow-derived dendritic cells (BMDCs) in a concentration-dependent manner.2 Topical administration of oclacitinib (0.1, 0.25, and 0.5%) reduces scratching behavior and ear edema, as well as decreases levels of IL-1β, IL-4, and IL-6 in ear skin, in a mouse model of allergic dermatitis induced by toluene-2,3-diisocyanate (TDI). Formulations containing oclacitinib have been used in the treatment of pruritus associated with allergic dermatitis and the control of atopic dermatitis in dogs.WARNING This product is not for human or veterinary use. | [References]
[1] A. J. GONZALES. Oclacitinib (APOQUEL®) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy[J]. Journal of veterinary pharmacology and therapeutics, 2014, 37 4: 317-324. DOI: 10.1111/jvp.12101
[2] TOMOKI FUKUYAMA. Topically Administered Janus-Kinase Inhibitors Tofacitinib and Oclacitinib Display Impressive Antipruritic and Anti-Inflammatory Responses in a Model of Allergic Dermatitis.[J]. Journal of Pharmacology and Experimental Therapeutics, 2015, 354 3: 394-405. DOI: 10.1124/jpet.115.223784 |
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