349438-38-6Alda 1

产品属性：

Cas No.349438-38-6

别名 N-(benzo[d][1,3]dioxol-5-ylmethyl)-2,6-dichlorobenzamide

化学名

分子式 C15H11Cl2NO3

分子量 324.16

溶解度 ≥ 15.15mg/mL in DMSO

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
IC50: N/A

Alda 1 is an activator of aldehyde dehydrogenase 2 (ALDH2).

Alda 1 increases activity of wild-type ALDH2*1 and variant ALDH2*2 (by ~2-fold and 11-fold respectively), Capable of partly restoring mutant ALDH2*2 activity, and protective against cardiac ischemia.

In vitro: In the present study , Alda-1 increased acetaldehyde oxidation by ALDH2*1 and ALDH2*2 approximately 1.5- and 6-fold, respectively, regarding GTN bioactivation and the effects of Alda-1. To similar extent, Alda-1 induced the esterase activities of both enzymes as the coenzyme NAD. NAD pronounced inhibition occurring at > 5mM, its the effect was biphasic. In the presence of 1 mM NAD, Alda-1 induced ALDH2*2-catalyzed ester hydrolysis 73-fold, whereas the NAD-induced activity of ALDH2*1 was inhibited on account of 20-fold increased inhibitory potency of NAD in the presence of the drug. ALDH2*2 displayed 7-fold lower GTN denitrating activity and GTN affinity than ALDH2*1, but the rate of nitric oxide formation was only reduced 2-fold. Soluble guanylate cyclase (sGC) activation was more pronounced than with wild type ALDH2 at saturating GTN. Alda-1 caused slight inhibition of GTN denitration, and in the presence of either variant, GTN-induced sGC activation was increased. The present results imply that established ALDH2 activities stimulated by Alda-1, which improved NAD binding but does not improve the GTN binding affinity of the Asian variant. In addition, an unexpected discrepancy between GTN reductase activity and sGC activation was revealed, which suggested that GTN denitration and bioactivation may display independent pathways of ALDH2-catalyzed GTN biotransformation [1].