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Lovastatin-d9 is intended for use as an internal standard for the quantification of lovastatin (Item No. 10010338) by GC- or LC-MS. Lovastatin is a fungal metabolite that has been found in A. terreus and an inhibitor of HMG-CoA reductase (Ki = 1.4 nM).1,2 It is also a prodrug form of the HMG-CoA reductase inhibitor lovastatin hydroxy acid (Item No. 10010339).2 Lovastatin (8 mg/kg per day) reduces plasma cholesterol levels in dogs. It suppresses TNF-induced NF-κB activation (IC50 = ~15 µM) and potentiates apoptosis in human myeloid leukemia cells.3 Lovastatin also increases cellular lipid peroxidation and decreases glutathione peroxidase 4 (GPX4) levels in cancer cells.4 Formulations containing lovastatin have been used in the treatment of hypercholesterolemia.WARNING This product is not for human or veterinary use. | [References]
[1] ENDO A. The discovery and development of HMG-CoA reductase inhibitors.[J]. Journal of Lipid Research, 1992, 33 11: 1569-1582.
[2] A W ALBERTS. Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1980, 77 7: 3957-3961. DOI: 10.1073/pnas.77.7.3957
[3] KWANG SEOK AHN Bharat B A Gautam Sethi. Reversal of chemoresistance and enhancement of apoptosis by statins through down-regulation of the NF-κB pathway[J]. Biochemical pharmacology, 2008, 75 4: Pages 907-913. DOI: 10.1016/j.bcp.2007.10.010
[4] VASANTHI S. VISWANATHAN. Dependency of a therapy-resistant state of cancer cells on a lipid peroxidase pathway[J]. Nature, 2017, 547 7664: 453-457. DOI: 10.1038/nature23007 |
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