| Identification | Back Directory | [Name]
YM-53601 | [CAS]
182959-33-7 | [Synonyms]
YM-53601 Exclusive
2-[(2E)-2-(1-azabicyclo[2.2.2]octan-3-ylidene)-2-fluoroethoxy]-9H-carbazole:hydrochloride
2-[(2E)-2-(1-azabicyclo[2.2.2]oct-3-ylidene)-2-fluoroethoxy]-9H-carbazole, monohydrochloride | [Molecular Formula]
C21H21FN2O.ClH | [MDL Number]
MFCD06411577 | [MOL File]
182959-33-7.mol | [Molecular Weight]
372.869 |
| Chemical Properties | Back Directory | [Melting point ]
236.5-237.2 °C | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 20 mg/ml; DMSO: 20 mg/ml; DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml; Ethanol: 2 mg/ml | [form ]
A crystalline solid | [color ]
Off-white to light brown |
| Hazard Information | Back Directory | [Uses]
YM-53601 is a squalene synthetase inhibitor. | [Definition]
ChEBI: YM-53601 is a member of carbazoles. | [Biological Activity]
Squalene synthase inhibitor.
YM-53601 is a cell penetrant and potent squalene synthase inhibitor inhibits cholesterol biosynthesis in rodents. YM-53601 lowers cholesterol levels and triglyceride levels better than HMG-CoA reductase inhibitor (prevastatin) and fibrate (fenofibrate.). | [in vivo]
YM-53601 suppresses cholesterol biosynthesis in rats (ED50, 32?mg/kg)[1].
YM-53601 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 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.
|
| [storage]
Store at -20°C |
|
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|