辛伐他汀，Simvastatin；Calbiochem®, ≥98% (HPLC)

A lipophilic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor that blocks Ras function through inhibition of farnesylation. Also inhibits glucose-induced Ca²⁺ signaling and insulin secretion by blocking L-type Ca²⁺ channels in rat islet β-cells. Inhibits cell proliferation of human smooth muscle cells. Note: this product is supplied in an inactive form and requires treatment with NaOH in EtOH followed by neutralization to pH 7.2 for activation.

A lipophilic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor that blocks Ras function through inhibition of farnesylation. Also inhibits glucose-induced Ca²⁺-signaling and insulin secretion by blocking L-type Ca²⁺ channels in rat islet β-cells. Inhibits cell proliferation of human smooth muscle cells. Note: This product is supplied in an inactive form and requires treatment with NaOH in ethanol followed by neutralization to pH 7.2 for activation.

 

Cell permeable: no

Primary Target
farnesylation

Product does not compete with ATP.

Reversible: no

 

Toxicity: Standard Handling (A)

 

Dissolve 50 mg in 1 ml in ethanol and add 0.813 ml of 1N NaOH. Adjust the pH to 7.2 by adding small quantities of 1N HCl before use.

 

Following reconstitution in ethanol-NaOH, aliquot and freeze (-20°C) Ethanol-NaOH solutions are stable for up to 1 month at -20°C. Neutralized solutions should be used immediately.

 

Yada, T., et al. 1999. Br. J. Pharmacol. 126, 1205.
Clutterbuck, R.D., et al. 1998. Br. J. Haematol. 102, 522.
Yokoyama, K., et al. 1998. Mol. Biochem. Parasitol. 94, 87.
Negre-Aminou, P., et al. 1997. Biochim. Biophys. Acta 1345, 259.
Vrtovsnik, F., et al. 1997. Kidney Int. 52, 1016.
Keyomarsi, K., et al. 1991. Cancer Res.51, 3602.

 

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany