Edasalonexent (CAT-1004)
(Synonyms: CAT-1004) 目录号 : GC31557
Edasalonexent (CAT-1004) (CAT-1004) 是一种口服生物可利用的 NF-κB 抑制剂。
Cas No.:1204317-86-1
Sample solution is provided at 25 µL, 10mM.
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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.
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]. |
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. | |
| Cas No. | 1204317-86-1 | SDF | |
| 别名 | CAT-1004 | ||
| Canonical 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 | ||
| 分子式 | C31H42N2O3 | 分子量 | 490.68 |
| 溶解度 | DMSO: 120 mg/mL (244.56 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.038 mL | 10.1899 mL | 20.3799 mL |
| 5 mM | 0.4076 mL | 2.038 mL | 4.076 mL |
| 10 mM | 0.2038 mL | 1.019 mL | 2.038 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet