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Cerivastatin sodium

Cat. No. M28423
Cerivastatin sodium Structure
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Biological Activity

Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.

Chemical Information
Molecular Weight 481.53
Formula C26H33FNNaO5
CAS Number 143201-11-0
Form Solid
Solubility (25°C) Water 100 mg/mL (ultrasonic and warming and heat to 60°C)
Storage -20°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Stephen P Adams, et al. Cochrane Database Syst Rev. Cerivastatin for lowering lipids

[2] A Cheng-Lai. Heart Dis. Cerivastatin

[3] W Mück. Clin Pharmacokinet. Clinical pharmacokinetics of cerivastatin

[4] H Bischoff, et al. Atherosclerosis. Preclinical review of cerivastatin sodium--a step forward in HMG-CoA reductase inhibition

[5] K J McClellan, et al. Drugs. Cerivastatin

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Keywords: Cerivastatin sodium supplier, HMG-CoA Reductase, inhibitors, activators


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