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. |
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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. |
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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 |
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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。 |