Edasalonexent

Modify Date: 2024-01-14 19:35:45

Edasalonexent Structure
Edasalonexent structure
Common Name Edasalonexent
CAS Number 1204317-86-1 Molecular Weight 490.677
Density 1.0±0.1 g/cm3 Boiling Point 716.8±60.0 °C at 760 mmHg
Molecular Formula C31H42N2O3 Melting Point N/A
MSDS N/A Flash Point 387.3±32.9 °C

 Use of Edasalonexent


Edasalonexent is an orally bioavailable NF-κB inhibitor.

 Names

Name edasalonexent
Synonym More Synonyms

 Edasalonexent Biological Activity

Description Edasalonexent is an orally bioavailable NF-κB inhibitor.
Related Catalog
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].
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].
Animal Admin Mice[1] Male mdx or WT mice are used. Drug treatment protocols entail feeding individually housed mice a specialty control chow or chow containing either CAT-1041 or Edasalonexent (0.75% w/w) ad libitum starting at 4 weeks of age. Average drug consumption typically ranges between 0.75 and 1 mg/g body weight per day. The 24-hour plasma exposure at this dosage is 450ng hr/mL for Edasalonexent[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. 2017 May;57(5):627-639.

 Chemical & Physical Properties

Density 1.0±0.1 g/cm3
Boiling Point 716.8±60.0 °C at 760 mmHg
Molecular Formula C31H42N2O3
Molecular Weight 490.677
Flash Point 387.3±32.9 °C
Exact Mass 490.319550
LogP 7.31
Vapour Pressure 0.0±2.4 mmHg at 25°C
Index of Refraction 1.554
Storage condition 2-8℃

 Synonyms

AF3Z6434KS
Benzamide, 2-hydroxy-N-[2-[[(4Z,7Z,10Z,13Z,16Z,19Z)-1-oxo-4,7,10,13,16,19-docosahexaen-1-yl]amino]ethyl]-
edasalonexent
N-{2-[(4Z,7Z,10Z,13Z,16Z,19Z)-4,7,10,13,16,19-Docosahexaenoylamino]ethyl}-2-hydroxybenzamide