Basic information Safety Supplier Related

YM-53601

Basic information Safety Supplier Related

YM-53601 Basic information

Product Name:
YM-53601
Synonyms:
  • 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
  • YM-53601 Exclusive
  • 9H-Carbazole, 2-[(2E)-2-(1-azabicyclo[2.2.2]oct-3-ylidene)-2-fluoroethoxy]-, hydrochloride (1:1)
  • (E)-2-(2-Fluoro-2-(quinuclidin-3-ylidene)ethoxy)-9H-carbazole hydrochloride
  • YM-53601 hydrochloride
CAS:
182959-33-7
MF:
C21H21FN2O.ClH
MW:
372.869
Mol File:
182959-33-7.mol
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YM-53601 Chemical Properties

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
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Safety Information

Safety Statements 
22-24/25
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YM-53601 Usage And Synthesis

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.

YM-53601Supplier

ChemStrong Scientific Co.,Ltd
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Shanghai YuanYe Biotechnology Co., Ltd.
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