Ro 48-8071 fumarate

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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 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.

Chemical Structure

Ro 48-8071 fumarate
CAS# 189197-69-1(fumarate)

Theoretical Analysis

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

Price and Availability

Size Price Availability Quantity
25.0mg USD 90.0 Same day
50.0mg USD 150.0 Same day
100.0mg USD 250.0 Same day
200.0mg USD 450.0 Same day
500.0mg USD 950.0 Same day
1.0g USD 1750.0 Same day
2.0g USD 3250.0 Same day
5.0g USD 5850.0 2 Weeks
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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 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+


Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 564.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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.

Additional Information

Related CAS#
CAS#189197-69-1(Ro 48-8071 fumarate salt);
CAS#161582-11-2 (Ro 48-8071 free base)