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• 產(chǎn)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

• 靶點： CETP

• 體外研究：
  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.

• 體內(nèi)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.

• 參考文獻：
  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

• 保存條件： 2-8℃

• 配置溶液濃度參考：
  

  	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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本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *