| 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 | [Uses]
ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC50 of 2.8 μM. | [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]
| [storage]
Store at -20°C | [References]
[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. DOI:10.1038/srep37798 |
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| Company Name: |
BOC Sciences
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| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
DC Chemicals
|
| Tel: |
021-58447131 13564518121 |
| Website: |
https://www.chemicalbook.com/ShowSupplierProductsList927327/0.htm |
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