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EN460

Cat. No. M14697
EN460 Structure
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Biological Activity

EN460 is a selective endoplasmic reticulum oxidation 1 (ERO1) inhibitor. EN460 (IC50 of 1.9 μM) interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation.

Chemical Information
Molecular Weight 460.79
CAS Number 496807-64-8
Solubility (25°C) DMSO 12.5 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shanna Hamilton, et al. Ero1α-Dependent ERp44 Dissociation From RyR2 Contributes to Cardiac Arrhythmia

[2] JianYu Yang, et al. ERO1L Promotes Hepatic Metastasis through Activating Epithelial-Mesenchymal Transition (EMT) in Pancreatic Cancer

[3] Junfeng Zhang, et al. Endoplasmic Reticulum stress-dependent expression of ERO1L promotes aerobic glycolysis in Pancreatic Cancer

[4] Zongyi Wang, et al. CYT997(Lexibulin) induces apoptosis and autophagy through the activation of mutually reinforced ER stress and ROS in osteosarcoma

[5] Werner J Geldenhuys, et al. High-content screen using zebrafish (Danio rerio) embryos identifies a novel kinase activator and inhibitor

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  Catalog
Abmole Inhibitor Catalog




Keywords: EN460 supplier, inhibitors, activators


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