182959-33-7
182959-33-7 structure
- Name: YM-53601
- Chemical Name: 2-[2-(1-azabicyclo[2.2.2]octan-3-ylidene)-2-fluoroethoxy]-9H-carbazole,hydrochloride
- CAS Number: 182959-33-7
- Molecular Formula: C21H22ClFN2O
- Molecular Weight: 372.86
- Catalog: Signaling Pathways Anti-infection HCV
- Create Date: 2016-06-14 06:12:29
- Modify Date: 2024-01-05 00:06:06
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YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo[1]. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent[2]. YM-53601 also is an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation[3].
| Name | 2-[2-(1-azabicyclo[2.2.2]octan-3-ylidene)-2-fluoroethoxy]-9H-carbazole,hydrochloride |
|---|---|
| Synonyms |
9H-Carbazole, 2-[[(2E)-2-(1-azabicyclo[2.2.2]oct-3-ylidene)-2-fluoroethyl]oxy]-, hydrochloride (1:1)
2-{[(2E)-2-(1-Azabicyclo[2.2.2]oct-3-ylidene)-2-fluoroethyl]oxy}-9H-carbazole hydrochloride (1:1) |
| Description | YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo[1]. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent[2]. YM-53601 also is an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation[3]. |
|---|---|
| Related Catalog | |
| In Vitro | YM-53601 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 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) potentiates the susceptibility of H35 cells to thapsigargin, lonidamine, and doxorubicin. YM-53601 (1 μM) reduces the mitochondrial cholesterol levels in both H35 and HepG2 cells[4]. 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 suppresses cholesterol biosynthesis in rats (ED50, 32 mg/kg)[1]. YM-53601 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 potentiates Doxorubicin-mediated hepatocellular carcinoma cells (HCC) growth arrest and cell death in vivo[4]. 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. |
| References |
| Molecular Formula | C21H22ClFN2O |
|---|---|
| Molecular Weight | 372.86 |
| Exact Mass | 372.140472 |
| PSA | 28.26000 |
| LogP | 5.38900 |