Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zosuquidar trihydrochloride (LY-335979 trihydrochloride) 是一种P-糖蛋白抑制剂,Ki 值为 59 nM。
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 |
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 31.9 mg/mL (50 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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