[CAS NO. 1204317-86-1] Edasalonexent
PRODUCTS SPECIFICATIONS [1204317-86-1]
DESCRIPTION [1204317-86-1]
Overview
| MDL | MFCD30533433 |
|---|---|
| Molecular Weight | 490.68 |
| Molecular Formula | C31H42N2O3 |
| SMILES | O=C(NCCNC(CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CC)=O)C1=CC=CC=C1O |
Summary
Edasalonexent (CAT-1004) is an orally bioavailable NF-κB inhibitor.
IC50 & Target
NF-κB [1]
In Vitro
Edasalonexent is an orally administered small molecule in which salicylic acid and docosahexaenoic acid (DHA) are covalently conjugated through an ethylenediamine linker and that is designed to synergistically leverage the ability of both of these compounds to inhibit NF-κB. Edasalonexent significantly inhibits NF-κB p65-dependent inflammatory responses as well as downstream proinflammatory genes modulated by p65 in the golden retriever duchenne muscular dystrophy (DMD) model [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The treatment of mdx mice with Edasalonexent for 20 weeks results in reduced susceptibility of the extensor digitorum longus muscle to eccentric contraction-induced injury [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03703882 | Catabasis Pharmaceuticals |
Muscular Dystrophy, Duchenne
|
October 2, 2018 | Phase 3 |
| NCT01670773 | Catabasis Pharmaceuticals |
Assessment of Mechanistic Blood Biomarkers in Healthy Humans
|
August 2012 | Phase 1 |
| NCT04543370 | Catabasis Pharmaceuticals |
Healthy
|
August 8, 2020 | Phase 1 |
| NCT02439216 | Catabasis Pharmaceuticals |
Muscular Dystrophy, Duchenne
|
April 2016 | Phase 1|Phase 2 |
| NCT01511900 | Catabasis Pharmaceuticals |
Type 2 Diabetes
|
December 2011 | Phase 1 |
| NCT03917719 | Catabasis Pharmaceuticals |
Duchenne Muscular Dystrophy
|
March 14, 2019 | Phase 3 |
Appearance
Oil
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 120 mg/mL ( 244.56 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0380 mL | 10.1899 mL | 20.3799 mL |
| 5 mM | 0.4076 mL | 2.0380 mL | 4.0760 mL |
| 10 mM | 0.2038 mL | 1.0190 mL | 2.0380 mL |
-
1.
References
- [1] Hammers DW, et al. Disease-modifying effects of orally bioavailable NF-κB inhibitors in dystrophin-deficient muscle. JCI Insight. 2016 Dec 22;1(21):e90341.
- [2] Donovan JM, et al. A Novel NF-κB Inhibitor, Edasalonexent (CAT-1004), in Development as a Disease-Modifying Treatment for Patients With Duchenne Muscular Dystrophy: Phase 1 Safety, Pharmacokinetics, and Pharmacodynamics in Adult Subjects. J Clin Pharmacol
