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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $2,120 | 8-10 weeks | |
50 mg | $2,780 | 8-10 weeks | |
100 mg | $3,700 | 8-10 weeks |
Description | Cerivastatin is a highly potent, well-tolerated, and orally active HMG-CoA reductase inhibitor (Ki: 1.3 nM/L). Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition with anti-cancer effect. Cerivastatin r |
In vitro | Cerivastatin (5-50 ng/mL; 3 days; MDA-MB-231 cells) induces a dose-dependent decrease in cell proliferation of MDA-MB-231 cells, achieving up to 40% inhibition at 25 ng/mL. At concentrations of 10-25 ng/mL for 18 hours, cerivastatin inhibits cell invasion through Matrigel. Cerivastatin (25 ng/mL; 4-36 hours) leads to NFκB inactivation dependent on RhoA inhibition, decreasing urokinase and metalloproteinase-9 expression, while increasing IκB levels. Additionally, cerivastatin (25 ng/mL; 18-36 hours) induces G1/S cell cycle arrest, delocalizes RhoA and Ras from membrane to cytosol, and causes morphological changes. Treatment with cerivastatin (25 ng/mL) for 18-36 hours markedly increases p21Waf1/Cip1 levels, and a 12-hour treatment increases p21 transcript levels, though G1/S arrest is not observed for an 18-hour incubation [1]. |
In vivo | Cerivastatin is highly bound to plasma proteins (99.5%), with an elimination half-life of 2-4 hours. Cerivastatin is well absorbed, reaching maximal plasma levels in 1-3 hours following oral dosing. Cerivastatin is metabolized predominantly in the liver to three polar metabolites. Plasma concentrations of all metabolites are substantially lower than those of the parent drug. Elimination of metabolites is via the urine (20-25%) and feces (66-73%), while essentially no parent compound is excreted [2]. |
Molecular Weight | 459.55 |
Formula | C26H34FNO5 |
Cas No. | 145599-86-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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