For research use only. Not for therapeutic Use.
Ro 48-8071 is an orally active cholesterol synthesis inhibitor or a 2,3-oxidosqualene:lanosterol cyclase (OSC) inhibitor. OSC (EC 5.4.99.7) represents a unique target for a cholesterol-lowering drug. Partial inhibition of OSC should reduce synthesis of lanosterol and subsequent sterols, and also stimulate the production of epoxysterols that repress HMG-CoA reductase expression, generating a synergistic, self-limited negative regulatory loop.
| Catalog Number | I009156 |
| CAS Number | 189197-69-1(fumarate) |
| Molecular Formula | C27H31BrFNO6 |
| Purity | ≥95% |
| Target | OSC inhibitor |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| IUPAC Name | (4-bromophenyl)-[2-fluoro-4-[6-[methyl(prop-2-enyl)amino]hexoxy]phenyl]methanone;(E)-but-2-enedioic acid |
| InChI | InChI=1S/C23H27BrFNO2.C4H4O4/c1-3-14-26(2)15-6-4-5-7-16-28-20-12-13-21(22(25)17-20)23(27)18-8-10-19(24)11-9-18;5-3(6)1-2-4(7)8/h3,8-13,17H,1,4-7,14-16H2,2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+ |
| InChIKey | XCYAYLWZCRGKDS-WLHGVMLRSA-N |
| SMILES | CN(CCCCCCOC1=CC(=C(C=C1)C(=O)C2=CC=C(C=C2)Br)F)CC=C.C(=CC(=O)O)C(=O)O |
| Reference | </br>1:Mafuvadze B, Liang Y, Hyder SM. Cholesterol synthesis inhibitor RO 48-8071 suppresses transcriptional activity of human estrogen and androgen receptor. Oncol Rep. 2014 Oct;32(4):1727-33. doi: 10.3892/or.2014.3332. Epub 2014 Jul 15. PubMed PMID: 25051231.</br>2:Liang Y, Besch-Williford C, Aebi JD, Mafuvadze B, Cook MT, Zou X, Hyder SM. Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071. Breast Cancer Res Treat. 2014 Jul;146(1):51-62. doi: 10.1007/s10549-014-2996-5. Epub 2014 May 31. PubMed PMID: 24878988.</br>3:Chuang JC, Valasek MA, Lopez AM, Posey KS, Repa JJ, Turley SD. Sustained and selective suppression of intestinal cholesterol synthesis by Ro 48-8071, an inhibitor of 2,3-oxidosqualene:lanosterol cyclase, in the BALB/c mouse. Biochem Pharmacol. 2014 Apr 1;88(3):351-63. doi: 10.1016/j.bcp.2014.01.031. Epub 2014 Jan 31. PubMed PMID: 24486573; PubMed Central PMCID: PMC3989900. |
