2-Hydroxy Atorvastatin Calcium Salt

Chemical Properties

White to Pale Yellow Solid

Uses

di(2-Hydroxy Atorvastatin) Calcium Salt is a metabolite of Atorvastatin Calcium Salt (A791750), a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia.

Biological Activity

2-Hydroxy atorvastatin calcium salt is a hydroxy metabolite of Atorvastatin calcium salt. Atorvastatin is a potent HMG-CoA reductase inhibitor with an IC50 value of 8 nM. It inhibits lipid hydroperoxide formation and copper sulfate-induced thiobarbituric acid reactive substances (TBARS) formation in 1,2-dilinoleoyl-sn-glycero-3-PC (DLPC) vesicles and human LDL, respectively, in a concentration-dependent manner. 2-Hydroxy Atorvastatin reduces cell death induced by oxygen-glucose deprivation (OGD) in primary rat cortical neurons and increases phosphorylation of cAMP-response-element-binding protein (CREB) in GABAergic neurons when used at a concentration of 600 nM following OGD.