For research use only. Not for therapeutic Use.
Lapaquistat (T-91485), a cholesterol biosynthesis inhibitor, is the active metabolite of Lapaquistat acetate (HY-16274). Lapaquistat can decrease statin-induced myotoxicity in lipid-lowering therapy[1].
Lapaquistat inhibits cholesterol biosynthesis in differentiated RD (rhabdomyosarcoma) cells, with an IC50 of 36 nM[1].
Lapaquistat potently inhibits cholesterol synthesis in RD cells, with an IC25 exceeded 100 μM[1].
Lapaquistat concentration-dependently inhibits cholesterol biosynthesis in human skeletal myocytes, with an IC50 of 45 nM[1].
After oral administration to rats, Lapaquistat acetate (HY-16274) is absorbed and rapidly hydrolyzed into a pharmacological active metabolite, Lapaquistat[1].
| Catalog Number | I017939 |
| CAS Number | 189059-71-0 |
| Synonyms | 2-[1-[2-[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-5H-4,1-benzoxazepin-3-yl]acetyl]piperidin-4-yl]acetic acid |
| Molecular Formula | C31H39ClN2O8 |
| Purity | ≥95% |
| InChI | InChI=1S/C31H39ClN2O8/c1-31(2,18-35)17-34-23-9-8-20(32)15-22(23)28(21-6-5-7-24(40-3)29(21)41-4)42-25(30(34)39)16-26(36)33-12-10-19(11-13-33)14-27(37)38/h5-9,15,19,25,28,35H,10-14,16-18H2,1-4H3,(H,37,38)/t25-,28-/m1/s1 |
| InChIKey | HDGUKVZPMPJBFK-LEAFIULHSA-N |
| SMILES | CC(C)(CN1C2=C(C=C(C=C2)Cl)C(OC(C1=O)CC(=O)N3CCC(CC3)CC(=O)O)C4=C(C(=CC=C4)OC)OC)CO |
| Reference | [1]. Nishimoto T, et al. Comparing myotoxic effects of squalene synthase inhibitor, T-91485, and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors in human myocytes. Biochem Pharmacol. 2003 Dec 1;66(11):2133-9. |
