S84696 |
Torcetrapib |
源叶(MedMol) | ≥98% |
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- 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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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)