唑喹达三盐酸盐|T6018|TargetMol

Zosuquidar trihydrochloride
167465-36-3

￥315 1mg 起订

￥449 2mg 起订

￥745 5mg 起订

上海更新日期：2026-05-08

TargetMol中国（陶术生物）

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联系人：邵小姐

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 唑喹达三盐酸盐

英文名称：: Zosuquidar trihydrochloride

CAS号：: 167465-36-3

品牌：: TargetMol

产地：: 美国

保存条件：: Store under nitrogen Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature.

纯度规格：: 99.97%

产品类别：: 抑制剂

货号：: T001|T6018

Product Introduction

Bioactivity

名称	Zosuquidar trihydrochloride
描述	Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a highly selective, potent competitive inhibitor of P-glycoprotein (P-gp, ABCB1) with a Ki value of 59 nM. Zosuquidar trihydrochloride exhibits antitumor activity and can be used in research on tumors such as leukemia.
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)
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.
体外活性	方法：在 P-gp 高表达的细胞系中加入 P-gp 抑制剂 Zosuquidar trihydrochloride （0.3 μM），同时加入 AVE9633 或 DM4 （3.125， 6.25， 12.5， 25， 50， 100 and 200 nM），AVE9633 处理 4 天，DM4 处理 3 天。单层细胞外排实验检测 P-gp 抑制。结果：Zosuquidar trihydrochloride 完全恢复了 P-gp 表达细胞对 AVE9633 和 DM4 的敏感性。[1] 方法：从 High-Five 昆虫细胞制备的表达野生型或突变型 P-gp 的粗膜。将膜蛋白与不同浓度抑制剂（zosuquidar， elacridar， tariquidar，浓度范围 0-100 μM）在 37°C 孵育，加入 5 mM ATP 启动反应，20 分钟后用 SDS 终止，通过比色法检测无机磷释放量。结果：在野生型 P-gp 中，Zosuquidar trihydrochloride 等抑制剂浓度依赖性抑制基础 ATP 酶活性，IC₅₀在 10-30 nM 范围。[2]
体内活性	方法：野生型小鼠通过颈动脉插管，以恒定流速(2.5 mL/min)向大脑灌注含有药物(imatinib， 0.05 - 50 μM; Zosuquidar trihydrochloride， 0.5 μM)的生理缓冲液。灌注结束后，立即处死小鼠，取脑组织测定药物浓度，计算脑摄取率。结果：Zosuquidar trihydrochloride 使 imatinib 脑摄取增加 2.5 倍。[3]
存储条件	Store under nitrogen Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 80.83 mg/mL (126.89 mM), Sonication is recommended.
关键字	Zosuquidar Trihydrochloride \| Zosuquidar (LY335979) \| Zosuquidar \| UCLA-P3.003VLB \| UCLA-P3 \| RS 33295-198 Trihydrochloride \| RS 33295-198 (D06387) \| RS 33295-198 \| P-gp (P-glycoprotein) \| P-gp \| Pgp \| P-glycoprotein \| P388/ADR \| P388 \| Multidrug resistance protein 1 \| MDR1 \| MCF7/ADR \| MCF7 \| LY-335979 Trihydrochloride \| LY335979 Trihydrochloride \| LY-335979 \| LY335979 \| LY 335979 Trihydrochloride \| LY 335979 \| K562 \| Inhibitor \| inhibit \| HL60 \| Cluster of differentiation 243 \| CEM/VLB100 \| CD243 \| CCRF-CEM \| anti-tumor activity \| AML \| acute myelogenous leukemia \| ABCB1 \| 2780AD \| 2780
相关产品	Bisdemethoxycurcumin \| Trifluoperazine dihydrochloride \| Tariquidar \| Cinchonine \| Glibenclamide \| Bifendate \| Verapamil hydrochloride \| Atazanavir \| Polyoxyethylene stearate \| Atazanavir sulfate \| Encequidar mesylate \| 1-piperoylpiperidine

唑喹达三盐酸盐;Zosuquidar 3HCl;Zosuquidar (LY335979) 3HCl;RS 33295-198 trihydrochloride;RS 33295-198 (D06387) 3HCl;LY-335979 trihydrochloride;TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

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