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

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

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ER-000444793

ER-000444793 Chemical Structure

CAS No. : 792957-74-5

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
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Based on 6 publication(s) in Google Scholar

Other Forms of ER-000444793:

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  • Pureté et documentation

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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].

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

Masse moléculaire

354.40

Formule

C23H18N2O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (141.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Pureté et documentation

Purity: 98.0%

Références
Test cellulaire
[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

Références

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8217 mL 14.1084 mL 28.2167 mL 70.5418 mL
5 mM 0.5643 mL 2.8217 mL 5.6433 mL 14.1084 mL
10 mM 0.2822 mL 1.4108 mL 2.8217 mL 7.0542 mL
15 mM 0.1881 mL 0.9406 mL 1.8811 mL 4.7028 mL
20 mM 0.1411 mL 0.7054 mL 1.4108 mL 3.5271 mL
25 mM 0.1129 mL 0.5643 mL 1.1287 mL 2.8217 mL
30 mM 0.0941 mL 0.4703 mL 0.9406 mL 2.3514 mL
40 mM 0.0705 mL 0.3527 mL 0.7054 mL 1.7635 mL
50 mM 0.0564 mL 0.2822 mL 0.5643 mL 1.4108 mL
60 mM 0.0470 mL 0.2351 mL 0.4703 mL 1.1757 mL
80 mM 0.0353 mL 0.1764 mL 0.3527 mL 0.8818 mL
100 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7054 mL
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Inquiry Information

Nom du produit:
ER-000444793
Cat. No.:
HY-100852
Quantité:
MCE Japan Authorized Agent: