Mevastatin or compactin is a cholesterol-lowering agent isolated from Penicillium citinium. It was the first discovered agent belonging to the class of cholesterol-lowering medications known as statins. During a search for antibiotic compounds produced by fungi in 1971, Akira Endo at Sankyo Co. (Japan) discovered a class of compounds that appeared to lower plasma cholesterol levels. Two years later, the research group isolated a compound structurally similar to hydroxymethylglutarate (HMG) that inhibited the incorporation of acetate. The compound was proposed to bind to the reductase enzyme and was named compactin. Mevastatin is a competitive inhibitor of HMG-Coenzyme A (HMG-CoA) reductase with a binding affinity 10,000 times greater than the HMG-CoA substrate itself. Mevastatin is a pro-drug that is activated by in vivo hydrolysis of the lactone ring. It has served as one of the lead compounds for the development of the synthetic compounds used today.
美伐他汀制备储备液:
浓度溶解体积质量
1mg
5mg
10mg
1mM
2.1032mL
10.5159mL
21.0318mL
5mM
0.4206mL
2.1032mL
4.2064mL
10mM
0.2103mL
1.0516mL
2.1032mL
50mM
0.0421mL
0.2103mL
0.4206mL
美伐他汀临床数据( 数据源于:http:// clinicaltrials.gov)
Conversion of different model animals based on BSA(Value based on data from FDA Draft Guidelines)
Animal A (mg/kg)=Animal B(mg/kg)multiplied by AnimalBm系数/AnimalAm系数 For example, to modify the dose of resveratrol uesd for a mouse(22.4mg/kg) to a dose based on the BSA for a rat, multiply 22.4mg/kg by the Km factor for a mouse and zhen divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2mg/kg