RO 48-8071
RO 48-8071 Basic information
- Product Name:
- RO 48-8071
- Synonyms:
-
- (4-Bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]methanone
- Methanone, (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]-, (2E)-2-butenedioate (1:1)
- OSC Inhibitor, Ro 48-8071 - CAS 189197-69-1 - Calbiochem
- RO 488071;RO48-8071;RO-48-8071
- CS-1750
- Ro 48-8071 fumarate salt
- (4-((6-(allyl(methyl)amino)hexyl)oxy)-2-fluorophenyl)(4-bromophenyl)methanone fumarate Ro48-8071
- (4-Bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]methanone (2E)-2-butenedioate (1:1)
- CAS:
- 189197-69-1
- MF:
- C23H27BrFNO2.C4H4O4
- MW:
- 564.45
- Product Categories:
-
- Inhibitors
- Mol File:
- 189197-69-1.mol
RO 48-8071 Chemical Properties
- Melting point:
- 90-92.7 °C
- storage temp.
- Inert atmosphere,Store in freezer, under -20°C
- solubility
- H2O: >5 mg/mL at ~60 °C
- form
- solid
- color
- white
- Water Solubility
- water: 5mg/mL
Safety Information
- Safety Statements
- 22-24/25
- WGK Germany
- 3
RO 48-8071 Usage And Synthesis
Uses
Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
Definition
ChEBI: A fumarate salt obtained by combining Ro 48-8071 with one molar equivalent of fumaric acid. An inhibitor of lanosterol synthase.
in vivo
Ro 48-8071 lowers LDL-C maximally appr 60% at 150 μmol/kg per day, with no further reduction up to 300 μmol/kg per day, leaving HDL-C unchanged at all doses in hamsters. Ro 48-8071 (≥00 μmol/kg per day) increases the amount of MOS in liver of hamsters. Ro 48-8071 (300 μmol/kg per day) remarkedly and significantly reduces VLDL secretion of hamsters[1]. Ro 48-8071 (5 or 20 mg/kg) significantly reduces in vivo tumor growth in mice, without weight loss of the mice. Furthermore, Ro 48-8071 at a concentration of 20 mg/kg, completely eradicates two of the 12 tumors being monitored in the mice in the timeframe tested[2]. Ro 48-8071 (20 mg/day/kg body weight) leads to a rapid and sustained inhibition (>50%) of cholesterol synthesis in the whole small intestine of BALB/c mice. Sterol synthesis is also reduced in the large intestine and stomach[4].
storage
Store at +4°C
References
[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. PMID:9162756
[2] Liang Y, et al. Cholesterol biosynthesis inhibitor RO 48-8071 suppresses growth of hormone-dependent and castration-resistant prostate cancer cells. Onco Targets Ther. 2016 May 30;9:3223-32 DOI:10.2147/OTT.S105725
[3] 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. DOI:10.1007/s10549-014-2996-5
[4] 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. DOI:10.1016/j.bcp.2014.01.031
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