1. Metabolic Enzyme/Protease
  2. Mitochondrial Metabolism
  3. ER-000444793

ER-000444793 

Cat. No.: HY-100852 Purity: >98.0%
Handling Instructions

ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC50 of 2.8 μM.

For research use only. We do not sell to patients.

ER-000444793 Chemical Structure

ER-000444793 Chemical Structure

CAS No. : 792957-74-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 327 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 660 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2340 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3540 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC50 of 2.8 μM.

IC50 & Target

IC50: 2.8 μM (mPTP)[1]

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[1].

Molecular Weight

354.40

Formula

C₂₃H₁₈N₂O₂

CAS No.

792957-74-5

SMILES

O=C(NC1=C(CC2=CC=CC=C2)C=CC=C1)C(C3=CC=CC=C3N4)=CC4=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (141.08 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8217 mL 14.1084 mL 28.2167 mL
5 mM 0.5643 mL 2.8217 mL 5.6433 mL
10 mM 0.2822 mL 1.4108 mL 2.8217 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

NFAT-RE-luc2 Jurkat cells are collected, centrifuged at 300 g for 5 minutes and re-suspended in serum-free RPMI-1640 media, plus supplements without antibiotic. Cell suspension (15,000 cells/20 μL) is added to each well of a solid black 384 well plate and incubated in the presence of compound for 20 hours at 37 °C. Alamar Blue is used and is added to each well at 2x concentration in media and reaction allowed to proceed for 4 hours at 37 °C. Fluorescence (ex. 540 nm/em. 590 nm) is recorded using Pherastar FS[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: >98.0%

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Keywords:

ER-000444793ER000444793ER 000444793Mitochondrial MetabolismInhibitorinhibitorinhibit

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ER-000444793
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HY-100852
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