ASK1-IN-1 是一种有效的、口服的、选择性的 ATP 竞争性凋亡信号调节激酶 1 (ASK1) 抑制剂，IC50 为 2.87 nM。
ASK1-IN-1 is an apoptosis signal regulating kinase 1 (ASK1) inhibitor extracted from patent WO2016025474A1, Compound 4.
ASK1-IN-1 dose-dependently decreases pulmonary arterial pressure and right ventricular (RV) hypertrophy in an in vivo model of pulmonary hypertension (PH). ASKl inhibition reduces hallmarks of pulmonary vascular disease including and not limited to reduce pulmonary vascular resistance (PVR), improve pulmonary pressure, decreased pulmonary vascular remodeling, improved vascular function, decrease maladaptive RV hypertrophy, and improve RV function. Inhibition of ASKl signaling may slow, prevent, and/or reverse pathological changes associated with PH. Plasma levels of B-type natriuretic peptide (BNP) are reduced by both doses of ASK1-IN-1: 0.1+0.05 for 0.1% and 0.1±0.1 ng/mL for 0.2%. Su/Hx rats treated with 0.1 % or 0.2% ASK1-IN-1 has a decreased number of completely muscularized arterioles (35.6% and 32.6%, respectively)[1].
参考文献:
[1]. Grant Raymond BUDAS, et al. Methods of treating pulmonary hypertension. WO2016025474A1.
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