YM-53601

• CAT Number: R065710
• CAS Number: 182959-33-7
• Molecular Formula: C21H22ClFN2O
• Molecular Weight: 372.868
• Purity: ≥95%
• Storage: -20°C
• IUPAC Name: 2-[2-(1-azabicyclo[2.2.2]octan-3-ylidene)-2-fluoroethoxy]-9H-carbazole;hydrochloride
• InChI: InChI=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
• InChIKey: JWXYVHMBPISIJQ-UHFFFAOYSA-N
• SMILES: C1CN2CCC1C(=C(COC3=CC4=C(C=C3)C5=CC=CC=C5N4)F)C2.Cl

Squalene synthase catalyzes the dimerization of two farnesyl pyrophosphate molecules to form the key cholesterol precursor, squalene. YM-<wbr></wbr>53601 inhibits squalene synthase activity in rat hepatic microsomes and human Hep-<wbr></wbr>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-<wbr></wbr>53601, causing a reduction in both cholesterol and triglyceride levels in plasma. Cholesterol-<wbr></wbr>reducing HMG-<wbr></wbr>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-<wbr></wbr>lowering properties of compounds such as YM-<wbr></wbr>53601 make squalene synthase inhibition an attractive alternative to the combination HMG-<wbr></wbr>CoA reductase inhibitor/fibrate therapy.

Reference

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. British Journal of Pharmacology 131, 63-70 (2000).