Item № 18113
CAS № 182959-33-7
Purity ≥98%
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500 µg $168.00 $0.00
1 mg $319.00 $0.00
5 mg $1,344.00 $0.00

Pricing updated 2015-10-04. Prices are subject to change without notice.

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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.1,2 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.1 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.

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Technical Information
Formal Name 2-[(2E)-2-(1-azabicyclo[2.2.2]oct-3-ylidene)-2-fluoroethoxy]-9H-carbazole, monohydrochloride
CAS Number 182959-33-7
Molecular Formula C21H21FN2O • HCl
Formula Weight 372.9
Purity ≥98%
Formulation A crystalline solid
InChI Code 1S/C21H21FN2O.ClH/c22-19(18-12-24-9-7-14(18)8-10-24)13-25-15-5-6-17-16-3-1-2-4-20(16)23-21(17)11-15;/h1-6,11,14,23H,7-10,12-13H2;1H/b19-18-;

WARNING - This product is not for human or veterinary use.

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Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
Stability 2 years
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References & Background Reading
Product Description References

1. Ugawa, T., Kakuta, H., Moritani, H., et al. YM-53601, a novel squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in several animal species. Br J Pharmacol 131 63-70 (2000).

2. Ishihara, T., Kakuta, H., Moritani, H., et al. Synthesis of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: Enzyme inhibition and effects on plasma lipid levels. Bioorg Med Chem 11 3735-3745 (2003).

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