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Oclacitinib

CAS No. : 1208319-26-9

MCE 站：Oclacitinib

产品活性：Oclacitinib 是一种新型 JAK 抑制剂。Oclacitinib 抑制 JAK1 *有效，IC₅₀ 为 10 nM。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt

作用靶点：JAK

In Vitro: Using isolated enzyme systems ａnd in vitro human or canine cell models, potency ａnd selectivity of Oclacitinib is determined against JAK family members ａnd cytokines that trigger JAK activation in cells. Inhibitory activity of Oclacitinib against JAK family members is determined in isolated enzyme systems. Oclacitinib inhibits JAK1, JAK2, JAK3, ａnd TYK2 by 50% at concentrations (IC₅₀＇s) of 10, 18, 99, ａnd 84 nM, respectively. Oclacitinib is most potent against the JAK1 enzyme, showing a 1.8-fold selectivity for JAK1 vs. JAK2 ａnd 9.9-fold selectivity toward JAK1 vs. JAK3. Oclacitinib inhibits JAK family members by 50% at concentrations (IC₅₀＇s) ranging from 10 to 99 nM ａnd does not inhibit a panel of 38 non-JAK kinases (IC₅₀＇s > 1000 nM). Oclacitinib also inhibits the function of JAK1-dependent cytokines involved in allergy ａnd inflammation (IL-2, IL-4, IL-6, ａnd IL-13) as well as pruritus (IL-31) at IC₅₀＇s ranging from 36 to 249 nM. Oclacitinib has minimal effects on cytokines that does not activate the JAK1 enzyme in cells (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC₅₀＇s > 1000 nM) .Topical treatment with Tofacitinib (0.1%) ａnd Oclacitinib (0.1%) leads to significant reduction of cell migration from mouse ear explants compared with vehicle-treated ears (all P < 0.05). The cell counts of MHC class II positive cells (that is, Langerhans cells) are significantly lower in vehicle-treated compared with each JAK inhibitortreated epidermis (all P < 0.01) .

In Vivo: Scratching bouts at the high dose in the Oclacitinib group are significantly less than in the vehicle-only group (P<0.01). Client-owned dogs (n=436) with moderate to severe owner-assessed pruritus ａnd a presumptive diagnosis of allergic dermatitis are enrolled. Dogs are randomized to either Oclacitinib at 0.4-0.6 mg/kg orally twice daily or an excipient-matched placebo. An enhanced 10 cm visual analog scale (VAS) is used to assess the severity of pruritus from day 0 to 7 ａnd to assess the severity of dermatitis on days 0 ａnd 7. Dogs can remain on the study for 28 days. Oclacitinib produces a rapid onset of efficacy within 24 h.

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