Description:
Oclacitinib maleate (PF-03394197) is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM. It does not inhibit a panel of 38 non-JAK kinases.
In vitro:
PF-03394197 inhibits JAK family members by 50% at concentrations ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases. PF-03394197 is most potent at inhibiting JAK1. PF-03394197 also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. PF-03394197 has minimal effects on cytokines which does not activate the JAK1 enzyme in cells.
In vivo:
PF-03394197 administered orally at a dose of 0.4–0.6 mg/kg twice daily is safe and efficacious in controlling the pruritus associated with allergic dermatitis. PF-03394197 provides itch relief within 24 h that persistes through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7.
JAK Inhibitors Related Products:
Ruxolitinib; Ruxolitinib phosphate; Tofacitinib; AZD1480; Momelotinib; Gandotinib; AZ960; Pacritinib; XL019; Upadacitinib; Decernotinib; Filgotinib; GLPG0634 analogue; FLLL32; AG-490 (Tyrphostin B42); NSC-42834; Itacitinib; Go6976; Baricitinib; Oclacitinib; WP1066