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S84696

Torcetrapib

源叶(MedMol) ≥98%
  • 英文名:
  • Torcetrapib
  • 别名:
  • 托彻普;(2R,4S)-4-[(3,5-双三氟甲基苄基)甲氧基甲酰氨基]-2-乙基-6-三氟甲基-3,4-二氢-2H-喹啉-1-羧酸乙酯
  • CAS号:
  • 262352-17-0
  • 分子式:
  • C26H25F9N2O4
  • 分子量:
  • 600.47
  • MDL:
  • MFCD09260777
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S84696-5mg ≥98% ¥620.00元 9 - - - EA 加入购物车
源叶(MedMol) S84696-10mg ≥98% ¥970.00元 10 - - - EA 加入购物车
源叶(MedMol) S84696-50mg ≥98% ¥3193.00元 10 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM
  • 靶点: CETP
  • 体外研究:
    The IC50 for Torcetrapib determined from the linear portion of the curves (25 to 80 nM) is 52 and 65 nM for the 3H-HDL and 14C-LDL cholesteryl ester transfer assays, respectively, using the specific activity-adjusted calculation, and 47 and 61 nM using a single exponential decay function. Torcetrapib (0, 0.5, 1, 5, and 10 μM) significantly reduced MCF-7 cells growth. Torcetrapib (0, 1, 5, 10, and 20 μM) does not inducing MCF-7 cells apoptosis. Torcetrapib (10 μM) binds to CETP with high affinity and down-regulates CETP expression. Cell Viability Assay Cell Line: MCF-7 cells Concentration: 0, 0.5, 1, 5, and 10 μM Incubation Time: 5 days Result: Significantly reduced cell growth. RT-PCR Cell Line: MCF-7 cells Concentration: 10 μM Incubation Time: 48 hours Result: Down-regulated CETP mRNA expression.
  • 体内研究:
    Torcetrapib (3, 10, or 30 mg/kg every day [qd]; oral gavage for 14 days) significantly increases high-density lipoprotein (HDL) cholesterol and reduceslow-density lipoprotein (LDL) cholesterol, and there is a tendency for Torcetrapib to reduce very-low-density lipoprotein (VLDL) cholesterol and triglycerides. Maximal increase in HDL cholesterol is 53% with Torcetrapib. Animal Model: Male Tg (B6; SJL-TgN (CETP)-TgN (ApoB100)) mice at 6 to 7 weeks of age Dosage: 3, 10, and 30 mg/kg Administration: Orally every day for 14 days Result: Significantly Increased HDL cholesterol by 27%, 24%, and 53% in the 3, 10, and 30 mg/kg groups compared to baseline, respectively, after 14 days of treatment.Significantly decreased LDL cholesterol by 44% and 35% at 10 and 30 mg/kg compared to baseline, respectively, after 14 days of treatment.
  • 参考文献:
    1. Ronald W Clark, et al. Raising high-density lipoprotein in humans through inhibition of cholesteryl ester transfer protein: an initial multidose study of torcetrapib.Arterioscler Thromb Vasc Biol. 2004 Mar;24(3):490-7. 2. Luke Esau, et al. Identification of CETP as a molecular target for estrogen positive breast cancer cell death by cholesterol depleting agents. Genes Cancer. 2016 Sep;7(9-10):309-322. 3. Michael K Hansen,et al. Selective CETP inhibition and PPARalpha agonism increase HDL cholesterol and reduce LDL cholesterol in human ApoB100/human CETP transgenic mice.J Cardiovasc Pharmacol Ther. 2010 Jun;15(2):196-202.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: 2-8℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.665 ml 8.327 ml 16.654 ml
    5 mM 0.333 ml 1.665 ml 3.331 ml
    10 mM 0.167 ml 0.833 ml 1.665 ml
    50 mM 0.033 ml 0.167 ml 0.333 ml
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