中文名 | ER-000444793 |
英文名 | ER-000444793 |
别名 | 化合物ER-000444793 N-(2-苄基苯基)-2-氧代-1,2-二氢喹啉-4-甲酰胺 |
英文别名 | ER-000444793 ER-000444793(ER000444793) N-(2-Benzylphenyl)-2-oxo-1,2-dihydroquinoline-4-carboxamide 4-Quinolinecarboxamide, 1,2-dihydro-2-oxo-N-[2-(phenylmethyl)phenyl]- |
CAS | 792957-74-5 |
化学式 | C23H18N2O2 |
分子量 | 354.4 |
溶解度 | DMSO: ≥ 100 mg/mL |
存储条件 | -20℃ |
体外研究 | 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 2+ -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 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 ER-000444793 in delaying mPT is independent of CypD functional inhibition. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.822 ml | 14.108 ml | 28.217 ml |
5 mM | 0.564 ml | 2.822 ml | 5.643 ml |
10 mM | 0.282 ml | 1.411 ml | 2.822 ml |
5 mM | 0.056 ml | 0.282 ml | 0.564 ml |
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