Oclacitinib-13C-d3 is intended for use as an internal standard for the quantification of oclacitinib 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.
|1. Gonzales, A.J., Bowman, J.W., Fici, G.J., et al. Oclacitinib (APOQUEL•) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J. Vet. Pharmacol. Ther. 37(4), 317-324 (2014).|2. Fukuyama, T., Ehling, S., Cook, E., et al. Topically administered Janus-kinase inhibitors ofacitinib and olacitinib dsplay impressive antipruritic and anti-inflammatory responses in a model of allergic dermatitis. J. Pharmacol. Exp. Ther. 354(3), 394-405 (2015).