Ro 48-8071 fumarate

• CAT Number: I002439
• CAS Number: 189197-69-1
• Molecular Formula: C₂₃H₂₇BrFNO₂.C₄H₄O₄
• Molecular Weight: 564.44
• Purity: ≥95%
• Target: Oxidosqualene cyclase inhibitor
• Solubility: DMSO: ≥ 55 mg/mL
• Storage: Inert atmosphere,Store in freezer, under -20°C
• IC50: 6.5 nM
• 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

Ro 48-8071 fumarate（Cat No.:I002439） is a potent inhibitor of oxidosqualene cyclase, displaying an IC50 value of approximately 6.5 nM. By targeting this enzyme, Ro 48-8071 fumarate disrupts the biosynthesis of cholesterol and other important sterols. Oxidosqualene cyclase is a key enzyme involved in the cyclization of oxidosqualene, a precursor molecule in the cholesterol biosynthesis pathway.

Reference

[1]. Morand OH, et al. Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin. J Lipid Res. 1997 Feb;38(2):373-90.
[2]. Abe I, et al. Photoaffinity labeling of oxidosqualene cyclase and squalene cyclase by a benzophenone-containing inhibitor. Biochemistry. 1998 Apr 28;37(17):5779-84.
[3]. Mafuvadze B, et al. Cholesterol synthesis inhibitor RO 48-8071 suppresses transcriptional activity of human estrogen and androgen receptor. Oncol Rep. 2014 Oct;32(4):1727-33.
[4]. Liang Y, et al. 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.
[5]. Chuang JC, et al. 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.