CAS 1204317-86-1|Edasalonexent

Introduction:Basic information about CAS 1204317-86-1|Edasalonexent, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameEdasalonexent
CAS Number1204317-86-1Molecular Weight490.677
Density1.0±0.1 g/cm3Boiling Point716.8±60.0 °C at 760 mmHg
Molecular FormulaC31H42N2O3Melting Point/
MSDS/Flash Point387.3±32.9 °C

Names

Nameedasalonexent
SynonymMore Synonyms

Edasalonexent BiologicalActivity

DescriptionEdasalonexent is an orally bioavailable NF-κB inhibitor.
Related CatalogResearch Areas >>Metabolic Disease
Target

NF-κB[1]

In VitroEdasalonexent 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 VivoThe 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 AdminMice[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

Density1.0±0.1 g/cm3
Boiling Point716.8±60.0 °C at 760 mmHg
Molecular FormulaC31H42N2O3
Molecular Weight490.677
Flash Point387.3±32.9 °C
Exact Mass490.319550
LogP7.31
Vapour Pressure0.0±2.4 mmHg at 25°C
Index of Refraction1.554
Storage condition2-8℃

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
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