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Zosuquidar trihydrochloride

Zosuquidar trihydrochloride

产品编号 T6018   CAS 167465-36-3
别名: 唑喹达三盐酸盐, Zosuquidar (LY335979) 3HCl, RS 33295-198 trihydrochloride, RS 33295-198 (D06387) 3HCl, Zosuquidar 3HCl, LY-335979 trihydrochloride

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) 是一种P-糖蛋白抑制剂,Ki 值为 59 nM。

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Zosuquidar trihydrochloride Chemical Structure
Zosuquidar trihydrochloride, CAS 167465-36-3
规格 价格/CNY 货期 数量
2 mg ¥ 518 现货
5 mg ¥ 877 现货
10 mg ¥ 1,339 现货
50 mg ¥ 3,230 现货
100 mg ¥ 4,730 现货
1 mL * 10 mM (in DMSO) ¥ 1,168 现货
其他形式的 Zosuquidar trihydrochloride:
产品目录号及名称: Zosuquidar trihydrochloride (T6018)
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选择批次  
纯度: 100%
纯度: 100%
纯度: 100%
纯度: 99.55%
纯度: 99.55%
纯度: 99.49%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.
靶点活性 P-gp:60 nM(Ki)
体外活性 LY335979 competitively inhibits equilibrium binding of [3H]vinblastine to Pgp by blocking [3H]azidopine photoaffinity labeling of the Pgp in CEM/VLB100 plasma membranes. [1] LY335979 alone shows the cytotoxicity to drug-sensitive and MDR cell lines with IC50 ranging from 6 μM-16 μM and produces its ability to completely reverse the resistance of the oncolytics (vinblastine, doxorubicin, or etoposide) to the MDR cell lines P388/ADR, MCF7/ADR, 2780AD, or UCLA-P3.003VLB at concentration of 0.1 and 0.5 μM. [1] LY335979 significantly restores drug sensitivity in P-gp-expressing leukemia cell lines including K562/HHT40, K562/HHT90, K562/DOX and HL60/DNR, and enhances the cytotoxicity of anthracyclines (daunorubicin, idarubicin, mitoxantrone) and gemtuzumab ozogamicin (Mylotarg) in primary AML blasts with active P-gp. [2] A latest paper indicates that LY335979 completely inhibits apically directed transport of (Z)-endoxifen in the ABCB1-transduced cells. [3]
体内活性 Zosuquidar trihydrochloride is only moderately active as an inhibitor of P-gp at the blood-brain. Zosuquidar trihydrochloride at an oral dose of 25 mg/kg increases the brain concentrations by about 2.5-fold at 1 h and 5-fold at 24 h after paclitaxel administrationbarrier[4]. Zosuquidar enhances the brain uptake of nelfinavir in a dose-dependent manner. Brain tissue/plasma nelfinavir concentration ratios increase from 0.06±0.03 in the absence of zosuquidar administration and 0.09±0.02 between 2 and 6 h after a 2 mg/kg intravenous dose of zosuquidar to 0.85±0.19 after 6h and 1.58±0.67 after 20 mg/kg zosuquidar[5].
激酶实验 ATPase Assay : P-Glycoprotein ATPase activity is measured by the liberation of inorganic phosphate from ATP. The assay is measured in a 96-well plate for 90 min at 37 °C. Membranes (8 μg-10 μg protein) are incubated in a total volume of 100 μL of buffer A containing 5 mM sodium azide, 1 mM ouabain, 1 mM EGTA, 3 mM ATP, an ATP regenerating system composed of 5 mM phosphoenolpyruvate, and 3.6 units/mL pyruvate kinase in the presence and absence of 1 mM sodium vanadate. Pgp-ATPase activity is defined as the vanadate-sensitive portion of the total ATPase activity. Plates are read 3 minutes after the addition of the detection solution. The absorbance is measured at 690 nm by a microtiter dish reader. A phosphate standard curve is used to calculate the μMol of phosphate formed. Samples are measured in triplicate.
细胞实验 Cell viability is determined using a modified 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye reduction method. Cells are harvested during logarithmic growth phase, and seeded in 96-well plates. The cells are then cultured for 72 hours in the presence of oncolytics with or without modulators. MCF-7 and MCF-7/ADR cells are incubated 24 hours before the addition of the drug with and without the LY335979. LY335979 is prepared as 2 mM DMSO stocks and added to wells to give final concentrations ranging from 0.05 to 5 μM. After 72 hours, 20 μL of freshly prepared 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (5 mg/mL in Dulbecco's PBS) is added to each well and incubated for 4 hours in a 37 °C incubator containing 5% CO2. Cells are pelleted in a Sorvall RT6000B centrifuge, 70 μL of medium is carefully removed from each well, and 100 μL of 2-propanol/0.04 N HC1 is added. Cells are resuspended 5-10 times with a Multipipettor or until no particulate matter is visible. Plates are immediately read on a Titertek Multiskan MCC/340 microplate reader Flow Laboratories with a test wavelength of 570 nm and a reference wavelength of 630 nm. Controls are measured in quadruplicate and modulators are measured in duplicate. Cytotoxicity analyses are also performed using the CeliTiter 96 AQueous assay kit.(Only for Reference)
别名 唑喹达三盐酸盐, Zosuquidar (LY335979) 3HCl, RS 33295-198 trihydrochloride, RS 33295-198 (D06387) 3HCl, Zosuquidar 3HCl, LY-335979 trihydrochloride
化合物与蛋白结合的复合物

T6018_2

Zosuquidar and UIC2 Fab complex of human-mouse chimeric ABCB1 (ABCB1HM)

分子量 636.99
分子式 C32H31F2N3O2·3HCl
CAS No. 167465-36-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 31.9 mg/mL (50 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5699 mL 7.8494 mL 15.6988 mL 39.2471 mL
5 mM 0.314 mL 1.5699 mL 3.1398 mL 7.8494 mL
10 mM 0.157 mL 0.7849 mL 1.5699 mL 3.9247 mL
20 mM 0.0785 mL 0.3925 mL 0.7849 mL 1.9624 mL
50 mM 0.0314 mL 0.157 mL 0.314 mL 0.7849 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Dantzig AH, et al. Cancer Res. 1996, 56(18), 4171-4179. 2. Tang R, et al. BMC Cancer. 2008, 8,51. 3. Iusuf D, J Pharmacol Exp Ther. 2011, 337(3), 710-717. 4. Kemper EM, et al. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol. 2004 Feb;53(2):173-8. 5. Anderson BD, et al. Dependence of nelfinavir brain uptake on dose and tissue concentrations of the selective P-glycoprotein inhibitor zosuquidar in rats. Drug Metab Dispos. 2006 Apr;34(4):653-9.
Chrysosplenetin Taxuspine X Encequidar mesylate Trifluoperazine Hernandezine PGP-4008 Alisol F 24-acetate Trifluoperazine dihydrochloride

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌药物库 抗癌临床化合物库 抗癌上市药物库 抗癌化合物库 已知活性化合物库 抗COVID-19化合物库 药物功能重定位化合物库 上市药物库 FDA上市及药典收录分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Zosuquidar trihydrochloride 167465-36-3 Membrane transporter/Ion channel Neuroscience P-gp LY335979 Trihydrochloride CEM/VLB100 唑喹达三盐酸盐 Pgp 2780AD Multidrug resistance protein 1 Zosuquidar Zosuquidar (LY335979) 3HCl CD243 Zosuquidar (LY335979) anti-tumor activity RS 33295-198 trihydrochloride LY 335979 P388/ADR LY335979 RS 33295-198 (D06387) 3HCl P-glycoprotein UCLA-P3.003VLB 2780 RS 33295-198 (D06387) LY-335979 Trihydrochloride RS 33295-198 Zosuquidar 3HCl ABCB1 LY 335979 Trihydrochloride MCF7 acute myelogenous leukemia MDR1 HL60 UCLA-P3 Zosuquidar Trihydrochloride P388 MCF7/ADR LY-335979 trihydrochloride RS 33295-198 Trihydrochloride CCRF-CEM K562 LY-335979 Inhibitor Cluster of differentiation 243 AML inhibit inhibitor

 

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