RPR107393 free base is a selective and potent inhibitor of squalene synthase (SQS) for the study of neurological disorders and endocrine and metabolic disorders.

Squalene synthase (rat liver microsomal):0.8 nM

RPR107393 free base is a highly selective squalene synthase inhibitor with sub-nanomolar activity. It inhibits rat liver microsomal squalene synthase with an IC50 value of 0.8 nM, and at a concentration of 1 μM, RPR107393 free base significantly inhibited cholesterol and triglyceride synthesis by 82.4% and 70.0%, respectively. [1][2]

One hour after oral administration of 10 mg/kg of RPR107393 free base, cholesterol synthesis was reduced by 92% with an ED50 value of approximately 5 mg/kg. Six hours later, cholesterol synthesis was reduced by 74% with the same dose of RPR107393 free base administered orally (time to 50% inhibition was approximately 7 hours). Hepatic cholesterol synthesis was inhibited by 82% after 10 hours of oral administration of 25 mg/kg RPR107393 free base, but the effect disappeared after 21 hours.
RPR107393 free base exhibited significant cholesterol-lowering effects in rats. Oral administration of RPR107393 free base 30 mg/kg twice daily reduced serum cholesterol by 35% after 2 days and nearly 50% after 3 days of treatment. [1]