Torcetrapib (CP-529414) 是一种选择性、有效的胆固醇酯转移蛋白 (CETP) 抑制剂。 在人血浆的抑制曲线中对CETP的最有效浓度为 37 nM。
| 生物活性 | Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having aCETPconcentration of 37 nM[1]. |
体外研究
(In Vitro) | The IC50for Torcetrapib determined from the linear portion of the curves (25 to 80 nM) is 52 and 65 nM for the3H-HDL and14C-LDL cholesteryl ester transfer assays, respectively, using the specific activity-adjusted calculation, and 47 and 61 nM using a single exponential decay function[1].
Torcetrapib (0, 0.5, 1, 5, and 10 μM) significantly reduced MCF-7 cells growth[2].
Torcetrapib (0, 1, 5, 10, and 20 μM) does not inducing MCF-7 cells apoptosis[2].
Torcetrapib (10 μM) binds to CETP with high affinity and down-regulates CETP expression[2].
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
(In Vivo) | 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[3].
| Animal Model: | Male Tg (B6; SJL-TgN (CETP)-TgN (ApoB100)) mice at 6 to 7 weeks of age[3] | | 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. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(166.54 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.6654 mL | 8.3268 mL | 16.6536 mL | | 5 mM | 0.3331 mL | 1.6654 mL | 3.3307 mL | | 10 mM | 0.1665 mL | 0.8327 mL | 1.6654 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.16 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.16 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
m.cnreagent.com