1. Metabolic Enzyme/Protease Anti-infection
  2. Farnesyl Transferase HCV
  3. YM-53601 free base

YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (YM-53601) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

YM-53601 free base Chemical Structure

YM-53601 free base Chemical Structure

CAS No. : 182959-28-0

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Description

YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo[1]. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent[2]. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation[3].

IC50 & Target

Target: Squalene synthetase[1]

In Vitro

YM-53601 free base inhibits squalene synthase activities in hepatic microsomes from several species of rat, hamster, guinea-pig, rhesus monkey, and human-derived HepG2 cell with IC50s of 90, 170, 46, 45, and 79 nM, respectively[1].
YM-53601 free base inhibits conversion of [3H]farnesyl diphosphate to [3H]squalene by hamster liver squalene synthase with the IC50 of 170 nM[2].
YM-53601 (1 μM) free base potentiates the susceptibility of H35 cells to thapsigargin, lonidamine, and doxorubicin. YM-53601 (1 μM) free base reduces the mitochondrial cholesterol levels in both H35 and HepG2 cells[4].

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

Cell Viability Assay[4]

Cell Line: H35 and HepG2 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Reduced the mitochondrial cholesterol levels in both H35 and HepG2 cells.
In Vivo

YM-53601 free base suppresses cholesterol biosynthesis in rats (ED50, 32 mg/kg)[1].
YM-53601 free base also reduces plasma non-HDL cholesterol levels in hamsters by approximately 70% at an oral dose of 50 mg/kg/day for 5 days[2].
YM-53601 free base potentiates Doxorubicin-mediated hepatocellular carcinoma cells (HCC) growth arrest and cell death in vivo[4]. "

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

Animal Model: Sprague-Dawley (SD) rats weighing 150-170 g[1]
Dosage: 6.25, 12.5, 25 or 50 mg/kg
Administration: Given a single p.o.
Result: Inhibited cholesterol biosynthesis from acetate in a dose-dependent manner in rats. The ED50 value for YM-53601 cholesterol biosynthesis inhibition is 32  mg/kg.
Animal Model: Five- to six-week-old male BALB/c athymic (nu/nu) nude mice[4]
Dosage: 15 mg/kg
Administration: 2 wk of daily treatment by p.o. gavage
Result: Significantly decreased the intratumor cholesterol levels.
Molecular Weight

336.40

Formula

C21H21FN2O

CAS No.
SMILES

F/C(COC1=CC(NC2=C3C=CC=C2)=C3C=C1)=C4CN5CCC/4CC5

Structure Classification
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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YM-53601 free base Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

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YM-53601 free base
Cat. No.:
HY-100313
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