CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model.
性状
Solid
IC50 & Target[1][2]
EC50: 35 μM (IRK), tyrosine kinase, Akt
体外研究(In Vitro)
CMX-2043 (15-250 mM; 10 min) has great peroxyl radical absorbance capacity.CMX-2043 (1.5 μM) weakly inhibits spleen tyrosine kinase (Syk) and tunica interna endothelial cell kinase (Tie2).CMX-2043 (50 μM; 45 min) activates Akt phosporylation via PI3K pathway in A549 cells.CMX-2043 (2.5 mM; 30 min) diminishes the rise in cytosolic calcium in a concentration-dependent manner in CHO-M1-WT3 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
CMX-2043 (50-200 mg/kg, 5 mL; p.o.; single dose) reduces myocardial ischemia-reperfusion injury (IRI) as measured by the myocardial infarct to area at risk (MI-AR) ratio and the incidence of arrhythmia. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
ClinicalTrial
参考文献
[1]. Alan S Lader, et al. CMX-2043 Mechanisms of Action In Vitro. J Cardiovasc Pharmacol. 2016 Sept;68:241-247. [2]. Baguisi A, et al. CMX-2043 Efficacy in a Rat Model of Cardiac Ischemia-Reperfusion Injury. J Cardiovasc Pharmacol Ther. 2016 Nov;21(6):563-569.
溶解度数据
In Vitro: DMSO : 20.83 mg/mL (51.24 mM; Need ultrasonic)配制储备液