Tyk2-IN-5 (compound 6) 是一个强效的、选择性的、具有口服活性的酪氨酸激酶 2 (Tyk2) 的抑制剂，作用于 JH2 结构域，其对 Tyk2 JH2 的 Ki 值为 0.086 nM，对 IFNα 的 IC50 值为 25 nM。能够高效抑制药效学老鼠模型中的 IFNγ 的产生，对老鼠关节炎模型具有完全的疗效。
货号:ajcx39480
CAS:1797432-62-2
分子式:C21H19FN8O2
分子量：434.43
溶解度:DMSO : 43.33 mg/mL (99.74 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model[1].

[1]. Liu C, et al. Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors. ACS Med Chem Lett. 2019 Feb 21;10(3):383-388.

Protocol:

Tyk2JH2 0.086nM(Ki)

IFNα 25nM(IC50)