MSC 2032964A

MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC₅₀ of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation^[1]. In Vitro:MSC 2032964A (10 μM) reveals a good metabolic stability with microsomal clearance <4 ml/min/mg, and a good apparent permeability^[1].
MSC 2032964A (10 μM) inhibits Lipopolysaccharide (LPS, HY-D1056)-induced ASK1 and p38 phosphorylation in mouse astrocytes^[1]. In Vivo:MSC 2032964A (5 mg/kg, p.o.) exhibits an oral bioavailability of 82%, a clearance of 1.1 L/kg/ h, a half-life of 5.2 h and a volume of distribution V_ss of 1.0 L/kg in SPrague Dawley rats^[1].
MSC 2032964A (30 mg/kg, p.o., once daily for 40 days) attenuates neurological symptoms in both spinal cord and optic nerve lesions, and thus ameliorates the MOG (35-55) (HY-P1240)-induced autoimmune encephalomyelitis in C57BL/6J mice model^[1].