ER-000444793

SKU: orb1217645

Description

ER-000444793 is a potent mitochondrial permeability transition pore (mPTP) opening inhibitor and it also inhibits mPTP (IC50: 2.8 μM).

Key Properties

• CAS Number: 792957-74-5
• MW: 354.4
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₈N₂O₂
• SMILES: O=C(NC1=C(CC2=CC=CC=C2)C=CC=C1)C(C3=CC=CC=C3N4)=CC4=O
• Target: mPTP
• Solubility: DMSO:50 mg/mL (141.08 mM; Need ultrasonic)

Bioactivity

• In Vitro:
  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 Ca2+-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 IC50 = 23 nM and SfA IC50 = 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

mPTP