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Mevastatin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mevastatin图片
CAS NO:73573-88-3
规格:≥98%
包装与价格:
包装价格(元)
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)390.51
FormulaC23H34O5
CAS No.73573-88-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 78 mg/mL (199.7 mM)
Water:<1 mg/mL
Ethanol: <1 mg/mL
SMILES CodeCC[C@H](C)C(O[C@H]1CCC=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(O3)=O)[C@@]12[H])=O
SynonymsML-236B; CS-500; CS 500; ML 236B; CS500; ML236B; Mevastatin, Compactin.
实验参考方法
In Vitro

In vitro activity: Mevastatin is a cholesterol-lowering agent isolated from Penicillium citinium. It reduces cholesterol synthesis to 50% of control at 0.01 pg/mL (26 nM). It is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. Mevastatin is a prodrug that is activated in vivo via hydrolysis of the lactone ring. The hydrolyzed lactone ring mimics the tetrahedral intermediate produced by the reductase allowing the agent to bind with 10,000 times greater affinity than its natural substrate. The bicyclic portion of mevastatin binds to the coenzyme A portion of the active site. Mevastatin increases levels of eNOS mRNA and protein, reduces infarct size, and improves neurological deficits in a dose- and time-dependent manner.


Kinase Assay: Mevastatin inhibits HMG-CoA reductase reversibly and competes with HMG-CoA. It shows a Ki value of about 1nM.


Cell Assay: Mevastatin inhibits sterol synthesis from acetate in various cells at low concentration of nanomolar. It also inhibits acetate incorporation with IC50 value of 1nM. Besides that, mevastatin completely suppresses the growth of L cells at 1.3μM. Mevastatin is also found to affect the cell cycle and change cell morphology in cultured fibroblasts.

In VivoAt doses of 5 and 20 mg/kg, mevastatin produces reduction of serum cholesterol levels at 3 hours after oral administration. It lowers the levels of serum cholesterol by approximately 30 % at a dose of 20 mg/kg. Mevastatin lowers hepatic production of cholesterol by competitively inhibiting HMG-CoA reductase. Cholesterol levels are reduced only after 28 days of treatment and does not correlate with infarct reduction. Baseline absolute cerebral blood flow is 30% higher after 14-day high-dose treatment.
Animal modelWistar-Imamichi male rats
Formulation & DosageDissolved in saline; 5, 20 mg/kg; p.o.
References

J Antibiot (Tokyo). 1976 Dec;29(12):1346-8; Stroke. 2001 Apr;32(4):980-6.