94061-83-3
Chemical Structure
Fluvastatin lactone
- CAS No.: 94061-83-3
- Formula:C24H24FNO3
- Molecular Weight:393.45
IUPAC Name: (4R,6S)-6-((E)-2-(3-(4-fluorophenyl)-1-isopropyl-1H-indol-2-yl)vinyl)-4-hydroxytetrahydro-2H-pyran-2-one
InChIKey: VPXDEUFAXJFWBG-MCBHFWOFSA-N
SMILES: O=C1C[C@H](O)C[C@@H](/C=C/C(N2C(C)C)=C(C3=CC=C(F)C=C3)C4=C2C=CC=C4)O1
Biological Activity: Fluvastatin lactone is the lactone form of Fluvastatin (HY-14664) detected in human plasma after administration. It competitively or mixed-type inhibits CYP2C9-catalyzed S-Warfarin 7-hydroxylation, and induces myotoxicity in a concentration- and time-dependent manner in rat and primary human skeletal muscle cells, reducing the number of surviving myotubes and causing morphological changes in myotubes. Fluvastatin lactone can be used for studies on myotoxicity and statin-induced myotoxicity[1][2].
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Fluvastatin lactone | Fluvastatin lactone is the lactone form of Fluvastatin (HY-14664) detected in human plasma after administration. It competitively or mixed-type inhibits CYP2C9-catalyzed S-Warfarin 7-hydroxylation, and induces myotoxicity in a concentration- and time-dependent manner in rat and primary human skeletal muscle cells, reducing the number of surviving myotubes and causing morphological changes in myotubes. Fluvastatin lactone can be used for studies on myotoxicity and statin-induced myotoxicity. | |||||||||||||||||||||
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References
- [1]. Skottheim IB, et al. Statin induced myotoxicity: the lactone forms are more potent than the acid forms in human skeletal muscle cells in vitro. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2008 Apr 23;33(4-5):317-25. [Content Brief]
- [2]. Shiozawa A, et al. Effects of acid and lactone forms of statins on S-warfarin 7-hydroxylation catalyzed by human liver microsomes and recombinant CYP2C9 variants (CYP2C9.1 and CYP2C9.3). Drug metabolism and pharmacokinetics. 2021 Feb;36:100364.
