product name Pravastatin sodium
Description: Pravastatin sodium (also known as CS-514 Sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM. It is natural product isolated from cultures of Nocardia autotrophica. Pravastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses by suppressing MHC II on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells.
References: Immunopharmacology. 1996 Aug;34(1):51-61; Br J Clin Pharmacol. 1994 Dec;38(6):513-9; Clin Cancer Res. 2007 Sep 15;13(18 Pt 1):5331-40.
446.51
Formula
C23H35O7.Na
CAS No.
81131-70-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 89 mg/mL (199.3 mM)
Water: 89 mg/mL (199.3 mM)
Ethanol: 12 mg/mL (26.9 mM)
Solubility (In vivo)
Synonyms
CS-514 Sodium
other peoduct :
| In Vitro |
In vitro activity: Pravastatin-Na at 10 μM inhibits the sterol synthesis at a level greater than 50% in PBMC. [1] Pravastatin produces relaxation of isolated aortic rings, with maximum vasorelaxations of 62.8% at 10 μM and latency of ~8 min. Pravastatin (< 10 μM) stimulates NOS activity and NO release within 10 min in cultured bovine aortic endothelial cells. L-arginine potentiates NO production in response to Pravastatin (< 10 μM) in cultured bovine aortic endothelial cells. Pravastatin results in a dose-dependent inhibition of macrophage cholesterol synthesis in human monocyte derived macrophages(HMDM), mouse peritoneal macrophages (MPM) and a J-774 A.1 macrophagelike cell lines. Small concentrations of pravastatin (< 0.19 μg/mL) increases the cellular cholesterol esterification rate after incubation with LDL, but higher concentrations (< 100 μg/mL) results in an inhibition of the esterification. Pravastatin (< 0.5 mM) decreases Rho/ROCK pathway activity in human colon and ileum explants, which leads to decreased CCN2 mRNA levels. Pravastatin (<1 mM) also induces CCN2 inhibition in primary human smooth muscle cells. Pravastatin (< 0.5 mM) decreases type I collagen and fibronectin mRNA levels in both human colon and ileum explants and primary human smooth muscle cells. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Pravastatin (40 mg, single dose) causes a reduction in cholesterol synthesis in human monocyte derived macrophages by 62% in healthy subjects and 47% in hypercholesterolaemic patients. Pravastatin (40 mg/day, 8 weeks) results in a 55% inhibition of cholesterol synthesis and a 57% increase in LDL degradation in hypercholesterolaemic patients. Pravastatin (30 mg/kg/d) results in decreased length of the dystrophic lesions by 34% and recovery of muscular structure in Male Wistar rats receiving irradiation, associated with decreased CCN2 level. |
| Animal model | Male Wistar rats receiving irradiation for 5 weeks |
| Formulation & Dosage | Dissolved in water; 30 mg/kg/day; oral administration |
| References | Immunopharmacology. 1996 Aug;34(1):51-61; Br J Clin Pharmacol. 1994 Dec;38(6):513-9; Clin Cancer Res. 2007 Sep 15;13(18 Pt 1):5331-40. |
