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ER-000444793

CAS No. : 792957-74-5

MCE 国际站：ER-000444793

产品活性：ER-000444793 是有效的线粒体通透性转换孔 (mPTP) 开放抑制剂。ER-000444793 抑制 mPTP， IC₅₀ 为 2.8 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Mitochondrial Metabolism

In Vitro: ER-000444793 is a small molecule, non-toxic mPTP inhibitor with a mechanism of action independent of CypD inhibition. ER-000444793 potently and dose-dependently inhibits Ca²⁺-induced mPT. ER-000444793 binds CypD, a CsA/CypD homogenous time-resolved fluorescence (HTRF) assay is used to study compound binding. Both CsA and SfA dose-dependently decrease HTRF signal, suggesting displacement of labelled CsA from rhCypD protein (CsA IC₅₀=23 nM and SfA IC₅₀= 5 nM). In contrast, ER-000444793 has no effect up to a concentration of 50 μM, indicating lack of displacement of labelled-CsA from rhCypD protein. Together, these data suggest the mechanism of ER-000444793 in delaying mPT is independent of CypD functional inhibition.

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