Description
RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8 nM.
Product information
CAS Number: 197576-78-6
Molecular Weight: 330.42
Formula: C22H22N2O
Chemical Name: 3-[4-(quinolin-6-yl)phenyl]-1-azabicyclo[2.2.2]octan-3-ol
Smiles: OC1(CN2CCC1CC2)C1C=CC(=CC=1)C1C=C2C=CC=NC2=CC=1
InChiKey: JICDBMXIQNEXKV-UHFFFAOYSA-N
InChi: InChI=1S/C22H22N2O/c25-22(15-24-12-9-20(22)10-13-24)19-6-3-16(4-7-19)17-5-8-21-18(14-17)2-1-11-23-21/h1-8,11,14,20,25H,9-10,12-13,15H2
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
RPR107393 is a selective squalene synthase inhibitor with subnanomolar potency. RPR107393 inhibits rat liver microsomal squalene synthase with an IC50 value of 0.8±0.2 nM (n=4). In the time-course study, cells are treated with ER-27856 (1 μM), RPR-107393 (10 μM), Atorvastatin (1 μM), or NB-598 (1 μM) for 2-24 h, and lipid biosynthesis during the last 2 h of the incubation is determined. RPR-107393 (10 μM) inhibits Cholesterol biosynthesis and reduces triglyceride biosynthesis. Similarly, 1 μM RPR-107393 inhibits Cholesterol and triglyceride biosynthesis by 82.4% and 70.0%, respectively.
In Vivo:
One hour after RPR107393 (10 mg/kg p.o.), Cholesterol biosynthesis is reduced by 92% with an approximate ED50 value of 5 mg/kg. Six hours after RPR107393 (10 mg/kg p.o.) administration, Cholesterol biosynthesis is reduced by 74% (the time for 50% inhibition is ~7 hr). An 82% inhibition of hepatic Cholesterol biosynthesis is observed 10 hr after RPR107393 (25 mg/kg p.o.), but the effect is no longer apparent at 21 hr. Inhibition of Cholesterol biosynthesis by Zaragozic acid or RPR107393 is associated with an accumulation of radiolabeled diacid products in the liver. RPR107393 is a potent Cholesterol-lowering agent in rats. RPR107393 (30 mg/kg p.o. b.i.d.) lowers serum Cholesterol by 35% after 2 days and by nearly 50% after 3 days of treatment.
Products are for research use only. Not for human use.
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