Mevastatin

Research use only, not for human use.

Mevastatin or compactin is a cholesterol-lowering agent isolated from Penicillium citinium.

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.

Cell Viability Assay Cell Line:Caco-2 cells Concentration:0 μM, 8 μM, 16 μM, 32 μM, 64 μM, 128 μM Incubation Time:5 days Result:Caused a dose-dependent decrease in cell number.Cell Cycle Analysis Cell Line:Caco-2 cells Concentration:32 μM, 64 μM, 128 μM Incubation Time:24 hours, 48 hours, 72 hours Result:Caused a dose-dependent increase of cells in G0/G1 and G2/M phases of the cell cycle.Western Blot Analysis Cell Line:Caco-2 cells Concentration:32 μM, 64 μM, 128 μM Incubation Time:72 hours Result:Resulted in a down-regulation of cyclin-dependent kinases (cdk) 4 and cdk 6 as well as cyclin D1.

Animal Model:Wild-type 129-SV/eVTAcBr male mice and eNOS-deficient male mice (18-22 g) with the filament model Dosage:2 mg/kg or 20 mg/kg Administration:Delivered via 7- or 14-day ALZET miniosmotic pumps implanted subcutaneously; daily; for 7, 14, or 28 days Result:Increased levels of endothelial nitric oxide synthase (eNOS) mRNA and protein, reduced infarct size, and improved neurological deficits in a dose- and time-dependent manner.

Compactin | CS 500 | L-637,312 | ML 236B | NSC 281245 | Statin I

Metabolic Enzyme/Protease

HMGCR

HMG-CoA reductase| CES1

Cancer

——

73573-88-3

390.51

C23H34O5

>98% (HPLC)

DMSO: 78mg/ml (199.74 mM);Water: <1mg/ml; Ethanol: <1mg/ml

CC[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

(1S,7S,8S,8aR)-8-(2-((2R,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)ethyl)-7-methyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl (S)-2-methylbutanoate

(-20℃)

With Ice Pack

≥ 2 years