2. Metabolic Enzyme/Protease
  3. Farnesyl Transferase
  4. RPR107393

RPR107393 is an orally active potent selective squalene synthase (SQS) inhibitor. RPR107393 inhibits rat liver microsomal squalene synthase with an IC50 value of 0.8 nM. RPR107393 reduces triglyceride biosynthesis by suppressing fatty acid biosynthesis via an increase in intracellular farnesol and its derivatives. RPR107393 reduces plasma cholesterol in rats and marmosets. RPR107393 can be used for metabolic disease research, such as hypercholesterolemia, hypertriglyceridemia and atherosclerosis[1][2].

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RPR107393

RPR107393 Chemical Structure

CAS No. : 190841-57-7

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RPR107393 Related Antibodies

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Description

RPR107393 is an orally active potent selective squalene synthase (SQS) inhibitor. RPR107393 inhibits rat liver microsomal squalene synthase with an IC50 value of 0.8 nM. RPR107393 reduces triglyceride biosynthesis by suppressing fatty acid biosynthesis via an increase in intracellular farnesol and its derivatives. RPR107393 reduces plasma cholesterol in rats and marmosets. RPR107393 can be used for metabolic disease research, such as hypercholesterolemia, hypertriglyceridemia and atherosclerosis[1][2].

IC50 & Target

IC50: 0.8±0.2 nM (rat liver microsomal squalene synthase)[1]
In Vitro

RPR107393 (10 min) is a potent inhibitor of rat liver microsomal squalene synthase, with IC50 values of 0.6 to 0.9 nM, and is inactive (3 % inhibition at 1 mM) against HMG-CoA reductase from rat liver microsomes[1].
RPR107393 (6 h) concentration-dependently inhibits cholesterol biosynthesis (IC50 = 880 nM) and triglyceride biosynthesis (IC50 = 410 nM) in rat hepatocytes[2].
RPR107393 (10 μM, 2-24 h) decreases the incorporation of [1-14C]acetic acid into lipids in rat hepatocytes in a time-dependent manner, with maximal inhibition of cholesterol and triglyceride biosynthesis occurring at 2 h and 24 h, respectively[2].
RPR107393 (1 μM, 4 h) inhibits cholesterol and triglyceride biosynthesis by 82.4 % and 70.0 % in rat hepatocytes, respectively, with the latter effect potentiated by MVL supplementation, suggesting a mechanism involving increased FPP derivatives[2].
RPR107393 (1-10 μM, 4 h) increases carnitine-dependent mitochondrial β-oxidation (by 26.5 % at 1 μM and 39.5 % at 10 μM), it reduces overall triglyceride biosynthesis through a β-oxidation-independent pathway[2].
RPR107393 (10 μM, 4 h) suppresses triglyceride biosynthesis in rat hepatocytes, reducing fatty acid and triglyceride synthesis by 67.7 % and 68.5 %, respectively, through inhibiting fatty acid synthesis rather than later metabolic stages[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RPR107393 Related Antibodies
In Vivo

RPR107393 (10, 25 and 30 mg/kg, p.o., sigle dose, b.i.d. for 2-4 days, or q.d. for 7 days) exerts potent hypolipidemic effects after oral administration in rats[1].
RPR107393 (20 mg/kg, p.o., b.i.d. or q.d. for 7 days) selectively lowers LDL cholesterol while maintaining a favorable HDL profile in marmosets[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (130-150 g)[1]
Dosage: 10 and 25 mg/kg
Administration: p.o., sigle dose
Result: Reduced cholesterol biosynthesis by 92 % at 10 mg/kg, with an approximate ED50 value of 5 mg/kg.
Reduced cholesterol biosynthesis by 74 % after 6 h, and the time for 50 % inhibition was ~7 hr at 10 mg/kg.
Inhibited hepatic cholesterol biosynthesis with an inhibition of 82 % at 25 mg/kg after 10 h, but the effect was no longer apparent at 21 h.
Inhibited cholesterol biosynthesis associated with an accumulation of radiolabeled diacid products in the liver.
Animal Model: Sprague-Dawley rats (130-150 g)[1]
Dosage: 30 mg/kg
Administration: p.o., b.i.d. for 2-4 days
Result: Lowered serum cholesterol by 35 % after 2 days and by nearly 50 % after 3 days.
The reduction in cholesterol was greater in the very low-density lipoprotein (VLDL) and low-density lipoprotein (LDL) fractions (66-88 %) than in the high-density lipoprotein (HDL) fraction (maximum, 35 %).
Reduced serum triglycerides by up to 70 %.
Induced hepatic microsomal HMG-CoA reductase activity by 12 to 34-fold.
Animal Model: Sprague-Dawley rats (130-150 g) given a chow diet or the same diet supplemented with 2 % cholestyramine (HY-104081)[1]
Dosage: 30 mg/kg
Administration: p.o., q.d. for 7 days
Result: The R and S enantiomers reduced serum cholesterol by 9 % and 24 %, and triglycerides by 46 % and 57 %, respectively.
Coadministration with 2 % cholestyramine in the diet reduced serum cholesterol by 49 %.
The R enantiomer administered alone did not lower serum LDL cholesterol, whereas coadministration with cholestyramine resulted in a 30 % reduction.
The reductions in LDL cholesterol with the S enantiomer in the absence and the presence of cholestyramine were 33 % and 61 %, respectively.
The reduction was greater in the VLDL and LDL fractions than in the HDL fraction.
Animal Model: Male common marmosets (Callithrix jacchus)[1]
Dosage: 20 mg/kg
Administration: p.o., b.i.d. for 7 days
Result: Reduced plasma cholesterol by 50 %.
The reduction in plasma cholesterol was selectively in the LDL fraction (≤50 %), whereas cholesterol in the HDL fraction was unchanged.
Produced a greater reduction in plasma cholesterol than Lovastatin (HY-N0504) or Pravastatin (HY-B0165) (which produced ≤31 % reduction at 50 mg/kg, b.i.d.).
Animal Model: Male common marmosets (Callithrix jacchus)[1]
Dosage: 20 mg/kg
Administration: p.o., q.d. for 7 days
Result: Both enantiomers reduced total plasma cholesterol by approximately 27 %.
The R and S enantiomers reduced LDL cholesterol by 50 % and 43 %, respectively.
Showed no significant changed in HDL cholesterol levels.
Molecular Weight

403.34

Formula

C22H24Cl2N2O
CAS No.
SMILES

OC1(C2=CC=C(C3=CC=C4N=CC=CC4=C3)C=C2)CN5CCC1CC5.Cl.Cl
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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RPR107393 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RPR107393190841-57-7RPR 107393RPR-107393Farnesyl TransferaseFtasesqualene synthaseSQSrat liver microsomaltriglyceride biosynthesisfarnesolratmarmosethypercholesterolemiahypertriglyceridemiaatherosclerosisInhibitorinhibitorinhibit

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