| Identification | Back Directory | [Name]
YM-53601 free base | [CAS]
182959-28-0 | [Synonyms]
YM-53601 free base 9H-Carbazole, 2-[2-(1-azabicyclo[2.2.2]oct-3-ylidene)-2-fluoroethoxy]-, (E)- (9CI) | [Molecular Formula]
C21H21FN2O | [MDL Number]
MFCD00951376 | [MOL File]
182959-28-0.mol | [Molecular Weight]
336.4 |
| Chemical Properties | Back Directory | [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) |
| Hazard Information | Back Directory | [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.
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| 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.
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| [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 |
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MedChemExpress
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