Cayman Chemical | Simvastatin | Description • MK 733 (CAS 79902-63-9)

10010344 Simvastatin

MK 733 (CAS 79902-63-9)

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Hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase is the rate-limiting enzyme in the cholesterol biosynthetic pathway and the target of the “statin” class of cholesterol-lowering drugs.¹ Simvastatin is a competitive inhibitor of HMG-CoA reductase with a K_i value of 0.12 nM for the hydrolyzed, open ring form of the molecule.² Simvastatin is marketed under the trade name Zocor^™ and is often prescribed in combination with ezetimibe (Zetia) to treat dyslipidemia. This drug combination is known commercially as Vytorin^™ or Inegy^™. After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg per day, plasma cholesterol levels were reduced by 33%.³ Simvastatin also suppresses TNF-induced NF-κB activation (IC₅₀ ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.⁴

1 Tobert, J.A. Lovastatin and beyond: The history of the HMG-CoA reductase inhibitors. Nature Reviews Drug Discovery 2 517-526 (2003).

2 Corsini, A., Maggi, F.M., Catapano, A.L. Pharmacology of competitive inhibitors of HMG-CoA reductase. Pharmacol Res 31(1) 9-27 (1995).

3 Chao, Y., Chen, J.S., Hunt, V.M., et al. Lowering of plasma cholesterol levels in animals by lovastatin and simvastatin. Eur J Clin Pharmacol 40 S11-S14 (1991).

4 Ahn, K.S., Sethi, G., Aggarwal, B.B. Reversal of chemoresistance and enhancement of apoptosis by statins through down-regulation of the NF-κB pathway. Biochem Pharmacol 75 907-913 (2008).

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Pricing updated 2010-03-16.
Prices are subject to change without notice.

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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.