product name Atorvastatin Calcium
Description: Atorvastatin Calcium is a potent and selective inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin is used primarily for lowering blood cholesterol and for prevention of events associated with cardiovascular disease. As with all statins, atorvastatin works by inhibiting HMG-CoA reductase, an enzyme found in liver tissue that plays a key role in production of cholesterol in the body.
References: J Clin Invest. 1998 Jun 15;101(12):2711-9; Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H457-66.
1155.34
Formula
2(C33H34FN2O5).Ca
CAS No.
134523-03-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (86.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
5% DMSO+castor oil: 23 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Atorvastatin inhibits pre-proET-1 mRNA expression in a concentration- and time-dependent fashion (60-70% maximum inhibition) and reduces immunoreactive ET-1 levels (25-50%), this inhibitory effect is maintained in the presence of oxidized LDL (1-50 mg/mL). Atorvastatin significantly reduces angiotensin II-induced and epidermal growth factor-induced ROS production in VSMCs. Atorvastatin downregulates mRNA expression of the NAD(P)H oxidase subunit nox1 in VSMCs, whereas p22phox mRNA expression is not significantly altered. Atorvastatin inhibits membrane translocation of rac1 GTPase, which is required for the activation of NAD(P)H oxidase. Atorvastatin (0.1 μM) significantly diminishes NF-κB activation induced by Ang II and TNF-α in mononuclear cells and VSMC. Atorvastatin (1 μM) diminishes MCP-1 expression induced by Ang II, TNF-α and is reversed by Mevalonate only in Ang II-stimulated cells. Atorvastatin (1 μM) diminishes IP-10 expression induced by Ang II and by TNF-α in VSMC, and this reduction is partially reversed by Mevalonate. Atorvastatin and Gemfibrozil metabolites, but not the parent drugs, are potent antioxidants against lipoprotein oxidation. Kinase Assay: Cell Assay: |
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| In Vivo | Atorvastatin reduces vascular mRNA expression of p22phox and nox1 and increased aortic catalase expression in statin-treated rats. Atorvastatin inhibits the increase of hsCRP serum levels in the cholesterol-fed rabbits. Atorvastatin inhibits the increase in osteopontin expression throughout the valve leaflet in the hypercholesterolemic aortic valves. |
| Animal model | |
| Formulation & Dosage | |
| References | J Clin Invest. 1998 Jun 15;101(12):2711-9; Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H457-66. |
