Identification | Back Directory | [Name]
ER-000444793 | [CAS]
792957-74-5 | [Synonyms]
ER-000444793 ER-000444793
(ER000444793) 4-Quinolinecarboxamide, 1,2-dihydro-2-oxo-N-[2-(phenylmethyl)phenyl]- | [Molecular Formula]
C23H18N2O2 | [MDL Number]
MFCD31544321 | [MOL File]
792957-74-5.mol | [Molecular Weight]
354.4 |
Hazard Information | Back Directory | [Biological Activity]
ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. It inhibits mPTP with IC50 of 2.8 μM. | [in vitro]
ER-000444793 is a small molecule, non-toxic mPTP inhibitor with a mechanism of action independent of CypD inhibition. It potently and dose-dependently inhibits Ca 2+ -induced mPT. It 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 IC 50 =23 nM and SfA IC 50 = 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 it in delaying mPT is independent of CypD functional inhibition. | [target]
IC50: 2.8 μM (mPTP) | [storage]
Store at -20°C |
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