YM-53601
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- Product name: YM-53601
- CAS: 182959-33-7
- MF: C21H21FN2O.ClH
- MW: 372.869
- EINECS:
- MDL Number:MFCD06411577
- 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)
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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
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
Safety Information
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Description
Squalene synthase catalyzes the dimerization of two farnesyl pyrophosphate molecules to form the key cholesterol precursor, squalene. YM-53601 inhibits squalene synthase activity in rat hepatic microsomes and human Hep-G2 cells with IC50 values of 90 and 79 nM, respectively. Cholesterol biosynthesis is inhibited in rats with an ED50 value of 32 mg/kg YM-53601, causing a reduction in both cholesterol and triglyceride levels in plasma. Cholesterol-reducing HMG-CoA reductase inhibitors, which have little effect on plasma triglyceride levels, are often paired with fibrates, which can have adverse effects, to treat hyperlipidemia. The lipid-lowering properties of compounds such as YM-53601 make squalene synthase inhibition an attractive alternative to the combination HMG-CoA reductase inhibitor/fibrate therapy.More related product prices
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