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YM-53601 Exclusive

Cayman Chemical Item Number 18113

(CAS 182959-33-7)

YM-53601 (CAS 182959-33-7)

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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.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.

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).

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
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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F/C(=C1/CN2CCC/1CC2)​/COc1ccc2c(c1)​[nH]​c1ccccc21Cl

Background Reading

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).

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).
Size Price Quantity Subtotal
500 µg $168.00 $0.00
1 mg $319.00 $0.00
5 mg $1,344.00 $0.00
10 mg $2,352.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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