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Torcetrapib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Torcetrapib图片
CAS NO:262352-17-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品名称
托彻普
CP-529414
产品介绍
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

600.47

性状

Solid

Formula

C26H25F9N2O4

CAS 号

262352-17-0

中文名称

托彻普;托斯瑞比

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.6654 mL8.3268 mL16.6536 mL
5 mM0.3331 mL1.6654 mL3.3307 mL
10 mM0.1665 mL0.8327 mL1.6654 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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。