RO 48-8071 fuMarate

  • CAS: 189197-69-1
  • MDL:
  • Product number:QC-11736
  • Molecular formula: C27H31BrFNO6
  • Purity: 99.1%
  • MW: 564.44
Size Price Stock
100mg $380 in stock
250mg $620 in stock
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Brief Description

Ro 48-8071 fumarate is an inhibitor of OSC(Oxidosqualene cyclase; IC50=6.5 nM) that has low-density lipoprotein (LDL) cholesterol lowering activity.
IC50 value: 6.5 nM
Target: Oxidosqualene cyclase inhibitor
in vitro: Ro 48-8.071 blocked human liver OSC and cholesterol synthesis in HepG2 cells in the nanomolar range; in cells it triggered the production of monooxidosqualene, dioxidosqualene, and epoxycholesterol [1]. Ro 48-8071 showed potent noncompetitive inhibition of bacterial squalene:hopene cyclase (SHC) from Alicyclobacillus acidocaldarius (IC50 = 9.0 nM, KI = 6.6 nM) and OSLC (IC50 = 40 nM, KI = 22 nM for homogeneous rat liver OSLC). Ro 48-8071 dose-dependently inhibited 17β-estradiol (E2)-induced ERα responsive luciferase activity (IC50 value, ~10 μM), under conditions that were non-toxic to the cells. Ro 48-8071 was less effective against ERβ-induced luciferase activity. Androgen receptor (AR) mediated transcriptional activity was also reduced by Ro 48-8071.
in vivo: Administration of Ro 48-8071 to mice with BT-474 tumor xenografts prevented tumor growth, with no apparent toxicity. Ro 48-8071 degraded ERα while concomitantly inducing the anti-proliferative protein ERβ. The lanosterol cyclase inhibitor, Ro 48-8071, when fed to BALB/c mice in a chow diet (20 mg/day/kg body weight), leads to a rapid and sustained inhibition (>50%) of cholesterol synthesis in the whole small intestine.

Solubility

DMSO 55 mg/ml

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Light yellow to yellow solid

All CEG Chemical products are intended for laboratory research use only.

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