YM-53601 free base
YM-53601 free base Basic information
- Product Name:
- YM-53601 free base
- Synonyms:
-
- YM-53601 free base
- 9H-Carbazole, 2-[2-(1-azabicyclo[2.2.2]oct-3-ylidene)-2-fluoroethoxy]-, (E)- (9CI)
- YM53601 free base,YM 53601 free base
- CAS:
- 182959-28-0
- MF:
- C21H21FN2O
- MW:
- 336.4
- Mol File:
- 182959-28-0.mol
YM-53601 free base Chemical Properties
- Boiling point:
- 541.2±40.0 °C(Predicted)
- Density
- 1.30±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 16.62±0.30(Predicted)
YM-53601 free base Usage And Synthesis
Uses
YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo[1]. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent[2]. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation[3].
in vivo
YM-53601 free base suppresses cholesterol biosynthesis in rats (ED50, 32 mg/kg)[1].
YM-53601 free base also reduces plasma non-HDL cholesterol levels in hamsters by approximately 70% at an oral dose of 50 mg/kg/day for 5 days[2].
YM-53601 free base potentiates Doxorubicin-mediated hepatocellular carcinoma cells (HCC) growth arrest and cell death in vivo[4]. "
| Animal Model: | Sprague-Dawley (SD) rats weighing 150-170?g[1] |
| Dosage: | 6.25, 12.5, 25 or 50?mg/kg |
| Administration: | Given a single p.o. |
| Result: | Inhibited cholesterol biosynthesis from acetate in a dose-dependent manner in rats. The ED50?value for YM-53601 cholesterol biosynthesis inhibition is 32? mg/kg. |
| Animal Model: | Five- to six-week-old male BALB/c athymic (nu/nu) nude mice[4] |
| Dosage: | 15 mg/kg |
| Administration: | 2 wk of daily treatment by p.o. gavage |
| Result: | Significantly decreased the intratumor cholesterol levels. |
References
[1] T Ugawa,?et al. YM-53601, a novel squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in several animal species. Br J Pharmacol.?2000 Sep;131(1):63-70. DOI:10.1038/sj.bjp.0703545
[2] Tsukasa Ishihara, et al. Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: enzyme inhibition and effects on plasma lipid levels. Bioorg Med Chem.?2003 Aug 15;11(17):3735-45. DOI:10.1016/s0968-0896(03)00336-5
[3] Eun-Mee Park,?et al. Farnesyl-diphosphate farnesyltransferase 1 regulates hepatitis C virus propagation. FEBS Lett.?2014 May 2;588(9):1813-20. DOI:10.1016/j.febslet.2014.03.043
[4] Joan Montero,et al.Mitochondrial cholesterol contributes to chemotherapy resistance in hepatocellular carcinoma. Cancer Res.?2008 Jul 1;68(13):5246-56. DOI:10.1158/0008-5472.CAN-07-6161
YM-53601 free baseSupplier
- Tel
- 028-81700200 18116577057
- 3003855609@qq.com
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Tel
- 4008200310
- marketing@tsbiochem.com
- Tel
- 13720134139 086-15871494362 13720134139
- orders@jknbiochem.com
- Tel
- 51288865780
- sales@biosynth.com