WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 510318
CAS#: 189197-69-1(fumarate)
Description: 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.
MedKoo Cat#: 510318
Name: Ro 48-8071 fumarate
CAS#: 189197-69-1(fumarate)
Chemical Formula: C27H31BrFNO6
Exact Mass:
Molecular Weight: 564.45
Elemental Analysis: C, 57.45; H, 5.54; Br, 14.16; F, 3.37; N, 2.48; O, 17.01
Related CAS #: 189197-69-1(fumarate) 161582-11-2 (free base)
Synonym: Ro 488071; Ro488071; Ro-488071; Ro 488071; Ro-488071; Ro488071; Ro 48-8071 fumarate;
IUPAC/Chemical Name: (4-((6-(allyl(methyl)amino)hexyl)oxy)-2-fluorophenyl)(4-bromophenyl)methanone fumarate
InChi Key: XCYAYLWZCRGKDS-WLHGVMLRSA-N
InChi Code: 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+
SMILES Code: O=C(C1=CC=C(OCCCCCCN(CC=C)C)C=C1F)C2=CC=C(Br)C=C2.O=C(O)/C=C/C(O)=O
Related CAS#
CAS#189197-69-1(Ro 48-8071 fumarate salt);
CAS#161582-11-2 (Ro 48-8071 free base)
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.
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.
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.
4: Peffley DM, Gayen AK, Morand OH. Down-regulation of 3-hydroxy-3-methylglutaryl coenzyme A reductase mRNA levels and synthesis in syrian hamster C100 cells by the oxidosqualene cyclase inhibitor [4'-(6-allyl-ethyl-amino-hexyloxy)-2'-fluoro-phenyl]-(4-bromophenyl)-me thanone (Ro 48-8071): comparison to simvastatin. Biochem Pharmacol. 1998 Aug 15;56(4):439-49. PubMed PMID: 9763219.
