|N-(苯并[d][1,3]二氧杂环戊烯-5-基甲基)-2,6-二氯苯甲酰胺|CsnPharm

CAS No.: 349438-38-6

N-(Benzo[d][1,3]dioxol-5-ylmethyl)-2,6-dichlorobenzamide Catalog No. CSN18233

Synonyms: Alda-1

Alda-1 is an ALDH2 agonist, cell-permeable activator of both the wild-type ALDH2*1 and the asian E487K mutant ALDH2*2 forms of mitochondrial aldehyde dehydrogenase 2 (mtALDH2).

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实验方案

技术信息

生物活性

描述Mitochondrial aldehyde dehydrogenase (ALDH2) plays roles in either toxic environmental aldehydes or organic ethanol metabolism as well as in disease therapy like cardiovascular disease. Alda-1 is an agonist that activates both wild-type ALDH2 and ALDH2*2 by bounding to the apo-form of them at the exit of the substrate tunnel and extends in toward the active site. At pH 7.5, the length and nature of 100 μM aldehydes that were acetaldehyde, propionaldehyde and butyraldehyde were activated in dependent ways with the concentrations of Alda-1 of 0, 3, 6, 20, 30 μM respectively. Alda-1 also antagonized daidzin inhibition of both ALDH2 and ALDH2*2 in a dependent way with concentrations of 10 μM. Furthermore, the combined activatory could significantly increase the effects of both Alda-1 and NAD⁺ on ester hydrolysis for the two enzymes, which inversely became antagonistic for ALDH2 if the concentration is very high^[1]. In male sprague-dawley rats study model with lung ischemia/reperfusion (I/R) injuries, 10 mg/kg Alda-1 treatment could significantly alleviate the I/R injury. The hepatic I/R could increase ROC which was reduced by Alda-1 treatment and damage ALDH2 activity without changing ALDH2 expression and the ALDH2 activity could also be increased by Alda-1. The accumulation of MDA and 4-HNE due to I/R could also be inhibited, indicating that Alda-1 could activate ALDH2 activity and thus diminish the accumulation of toxic products. Furthermore, Alda-1 was proved to reduce the inflammatory response, ROS level, cell viability and mitochondrial membrane potential^[2]. In sum, Alda-1 could enhance the catalytic ALDH2 activity by 2-times with EC₅₀ of 20 μM and inhibit 4-HNE-induced inactivation of ALDH2. 8 mg/kg Injection of Alda-1 could decrease creatine kinase release into the blood by 50%^[3].
动物研究
剂量
Rat: 12.5 mg/kg - 50 mg/kg^[4] (i.p.), 1.5 mg/kg^[5] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Rat: 12.5 mg/kg - 50 mg/kg^[4] (i.p.), 1.5 mg/kg^[5] (i.p.)
给药途径	i.p.

[1] Perez-Miller S, Younus H, et al. Alda-1 is an agonist and chemical chaperone for the common human aldehyde dehydrogenase 2 variant. Nat Struct Mol Biol. 2010;17(2):159-64.
[2] Zhang T, Zhao Q, et al. Alda-1, an ALDH2 activator, protects against hepatic ischemia/reperfusion injury in rats via inhibition of oxidative stress. Free Radic Res. 2018;52(6):629-638.
[3] Chen CH, Ferreira JC, et al. Targeting aldehyde dehydrogenase 2: new therapeutic opportunities. Physiol Rev. 2014;94(1):1-34.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0849 mL
- 15.4245 mL
- 30.8490 mL
- 5 mM
- 0.6170 mL
- 3.0849 mL
- 6.1698 mL
- 10 mM
- 0.3085 mL
- 1.5424 mL
- 3.0849 mL

技术信息

CAS号

349438-38-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H11Cl2NO3

运输

蓝冰

分子量

324.16

别名

Alda-1

溶解度

DMSO	65.0 mg/mL (200.5 mM)
Water	Insoluble
Ethanol	12.0 mg/mL (37.0 mM)

动物实验配方

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N-(Benzo[d][1,3]dioxol-5-ylmethyl)-2,6-dichlorobenzamide Catalog No. CSN18233

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