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。

ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC 50 of 2.8?μM.

Solid

IC50: 2.8?μM (mPTP)

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 Ca-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. has not independently confirmed the accuracy of these methods. They are for reference

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Briston T, et al. Identification of ER-000444793, a Cyclophilin D-independent inhibitor of mitochondrial permeability transition, using a high-throughput screen in cryopreserved mitochondria. Sci Rep. 2016 Nov 25;6:37798.

In Vitro: DMSO : 50 mg/mL (141.08 mM; Need ultrasonic)配制储备液