Cerivastatin sodium

SKU: orb1710087

Description

Cerivastatin sodium is a highly potent, orally active inhibitor of HMG-CoA reductase, demonstrating lipid-lowering effects by reducing LDL cholesterol. It is utilized in research on hyperlipidemia and has been investigated in vitro and in vivo for its potential anticancer properties.

Research Area

Cell Biology, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 143201-11-0
• MW: 481.53
• Purity: >99.99% (May vary between batches)
• Formula: C₂₆H₃₃FNNaO₅
• SMILES: [O-]C(C[C@H](O)C[C@H](O)/C=C/C1=C(C(C)C)N=C(C(C)C)C(COC)=C1C2=CC=C(C=C2)F)=O.[Na+]
• Target: Opioid Receptor,HMG-CoA Reductase,Ferroptosis
• Solubility: DMSO:80 mg/mL (166.14 mM);H2O:80 mg/mL (166.14 mM)

Bioactivity

• Target IC50:
  HMG-CoA reductase:ki:1.3 nM/L
• In Vivo:
  Cerivastatin sodium is well absorbed, reaching maximum plasma concentrations within 1-3 hours after oral administration. In the circulation, it is highly bound to plasma proteins (99.5%) and has an elimination half-life of 2-4 h. Cerivastatin sodium is metabolized primarily by the liver to three polar metabolites. Two of these metabolites are somewhat active, but much less so than the prodrug, while the third metabolite is inactive. Plasma concentrations of these metabolites are much lower than those of the prodrug. The metabolites are excreted primarily in the urine (20-25%) and feces (66-73%), with little detectable excretion of the unchanged prodrug.
• In Vitro:
  Cerivastatin sodium 5-50 ng/mL treatment induces a dose-dependent decrease in cell proliferation of MDA-MB-231 cells (up to 40% inhibition at 25 ng/mL), and 10-25 ng/mL Cerivastatin sodium inhibits invasion of MDA-MB-231 cells through Matrigel. 25 ng/mL Cerivastatin sodium delocalizes RhoA and Ras from the membrane to the cytosol and induces morphological changes, and induces a marked increase in the level of p21Waf1/Cip1. This treatment increases the p21 transcript in MDA-MB-231 cells, and induces inactivation of NFκB, in a RhoA inhibition-dependent manner, resulting in a decrease in urokinase and metalloproteinase-9 expression, and concomitantly increases IκB.

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HMGCoA Reductase, HMG-CoA Reductase, HMG-CoA reductase, HMGCoAReductase, Ferroptosis, NOP receptor, OpioidReceptor, Opioid Receptor, Cerivastatin sodium, BAY W 6228 sodium

Compound Identifiers

PubChem CID

23663992