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ChemicalBook--->CAS DataBase List--->792957-74-5

792957-74-5

792957-74-5 Structure

792957-74-5 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : ≥ 100 mg/mL (282.17 mM)
[form ]

Solid
[color ]

Off-white to light yellow
Hazard InformationBack 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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