Biological Activity

Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent).

Product Citations

• 

  Pak J Pharm Sci. 2016 May;29(3 Suppl):1043-51.

  Chromatographic resolution of drug analogues: 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors (statins)
  Lovastatin purchased from AbMole

Customer Product Validations & Biological Datas

	Source	Pak J Pharm Sci (2016). Figure 1. Lovastatin (Abmole Bioscience)
	Method	HPLC chromatogram
	Cell Lines
	Concentrations	200μg/ml
	Incubation Time
	Results	The results summarized in (table 1) obtained for pravastatin, rosuvastatin, pitavastatin, atorvastatin, fluvastatin, lovastatin and simvastatin were comparable with the corresponding labeled amounts.

Chemical Information

Molecular Weight	404.54
Formula	C24H36O5
CAS Number	75330-75-5
Solubility (25°C)	DMSO ≥ 60 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nazish Sayed, et al. Clinical trial in a dish using iPSCs shows lovastatin improves endothelial dysfunction and cellular cross-talk in LMNA cardiomyopathy

[2] Yaru Zhang, et al. An overview on the biosynthesis and metabolic regulation of monacolin K/lovastatin

[3] Zixiao Xiong, et al. An overview of the bioactivity of monacolin K / lovastatin

[4] Kelly C L Mulder, et al. Lovastatin production: From molecular basis to industrial process optimization

[5] F P Zeller, et al. Lovastatin for hypercholesterolemia