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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- CAS. Nr.: 94061-83-3
- Formel: C24H24FNO3
- Molecular Weight:393.45
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
CYP2C9 |
In Vitro
Fluvastatin lactone (0-100 µM; 20 min) inhibits CYP2C9-catalyzed S-warfarin 7-hydroxylation in HLMs and recombinant CYP2C9.1/CYP2C9.3, with Ki values of 0.671 µM (HLMs), 0.687 µM (rCYP2C9.1), and 1.76 µM (rCYP2C9.3)[2].
Fluvastatin lactone (100-400 μM; 24-72 h) induces myotoxicity in primary human skeletal muscle cells (myotubes), is 26-fold more potent than Fluvastatin acid at 400 μM, and at 100 μM causes nearly complete loss of viable myotubes within 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 94061-83-3
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Molecular Weight 393.45
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Formel C24H24FNO3
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Fluvastatin lactone Related Classifications
HY-137213 Related Classifications
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