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

YM-53601 free base 是一种角鲨烯合酶 (squalene synthase) 抑制剂，可降低体内血浆胆固醇和甘油三酯水平。YM-53601 free base 抑制源自人肝癌细胞的角鲨烯合酶，IC50 为 79 nM。可用作降脂剂[2] 。YM-53601 free base 还是法呢基二磷酸法呢基转移酶 1 (FDFT1) 酶活性的抑制剂，可抑制 HCV 传播。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 YM-53601 通常具有更好的水溶性和稳定性。

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YM-53601 free base Chemical Structure

YM-53601 free base Chemical Structure

CAS No. : 182959-28-0

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YM-53601 free base 的其他形式现货产品:

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YM-53601 free base 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
体外研究
(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].

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

YM-53601 free base 相关抗体:

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.
体内研究
(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]. "

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.
分子量

336.40

Formula

C21H21FN2O
CAS 号
结构分类
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

YM-53601 free base 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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.

Keywords:

YM-53601182959-28-0YM53601YM 53601Farnesyl TransferaseHCVFtaseHepatitis C virusSqualenesynthaseplasmacholesteroltriglyceridehepatomafarnesyl-diphosphatefarnesyltransferaseFDFT1hypocholesterolemicHMG-CoAreductasehypercholesterolemiaInhibitorinhibitorinhibit

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