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Simvastatin acid

Cat. No. M27949
Simvastatin acid Structure
Synonym:

Tenivastatin

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Quality Control & Documentation
Biological Activity

Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin, is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.

Chemical Information
Molecular Weight 436.58
Formula C25H40O6
CAS Number 121009-77-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Anssi J H Mykkänen, et al. Clin Pharmacol Ther. Genomewide Association Study of Simvastatin Pharmacokinetics

[2] Yu Zhang, et al. Biomed Chromatogr. A validated LC-MS/MS method for simultaneous quantification of simvastatin and simvastatin acid in beagle plasma: Application to an absolute bioavailability study

[3] Amandla Atilano-Roque, et al. Toxicol In Vitro. Characterization of simvastatin acid uptake by organic anion transporting polypeptide 3A1 (OATP3A1) and influence of drυg-drυg interaction

[4] Dan Xu, et al. Acta Pharmacol Sin. Decreased exposure of simvastatin and simvastatin acid in a rat model of type 2 diabetes

[5] A Kalliokoski, et al. Br J Pharmacol. Impact of OATP transporters on pharmacokinetics

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Keywords: Simvastatin acid, Tenivastatin supplier, HMG-CoA Reductase, inhibitors, activators


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