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Edasalonexent(CAT-1004)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Edasalonexent(CAT-1004)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Edasalonexent (CAT-1004) (CAT-1004) 是一种口服生物可利用的 NF-κB 抑制剂。

Animal experiment:

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].

产品描述

Edasalonexent is an orally bioavailable NF-κB inhibitor.

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].

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].

[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.