ER-000444793 是一种线粒体通透性转换孔开放抑制剂。它能够抑制 mPTP,IC50=2.8 μM。
产品描述
ER-000444793 is a potent mitochondrial permeability transition pore (mPTP) opening inhibitor and it also inhibits mPTP (IC50: 2.8 μM).
体外活性
ER-000444793 is a small molecule and non-toxic mPTP inhibitor. It also has a mechanism of action independent of CypD inhibition. Both CsA and SfA dose-dependently reduce HTRF signal, showing the displacement of labeled CsA from rhCypD protein (CsA IC50=23?nM and SfA IC50=?5?nM). However, ER-000444793 has no effect up to a concentration of 50?μM, showing be short of displacement of labelled-CsA from rhCypD protein. 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. These data display the mechanism of ER-000444793 in delaying mPT is independent of CypD functional inhibition[1].
Cas No.
792957-74-5
分子式
C23H18N2O2
分子量
354.4
储存和溶解度
DMSO:50 mg/mL (141.08 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years