唑喹达三盐酸盐|T6018|TargetMol

Zosuquidar trihydrochloride
167465-36-3

￥315 1mg 起订

￥745 5mg 起订

￥1070 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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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：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.55%

产品类别：: 抑制剂

货号：: T6018

Product Introduction

Bioactivity

名称	Zosuquidar trihydrochloride
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.
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	Zosuquidar通过阻断[3H]azidopine光亲和标记CEM/VLB100质膜中的Pgp，竞争性抑制[3H]vinblastine与Pgp的平衡结合。[1] Zosuquidar单独对药物敏感和多药抗性（MDR）细胞系表现出具有IC50在6 μM至16 μM范围内的细胞毒性，并且能够以0.1及0.5 μM浓度完全逆转MDR细胞系P388/ADR、MCF7/ADR、2780AD或UCLA-P3.003VLB对化疗化合物（vinblastine、doxorubicin或etoposide）的抗性。[1] Zosuquidar显著恢复表达P-gp的白血病细胞系（包括K562/HHT40、K562/HHT90、K562/DOX和HL60/DNR）对药物的敏感性，并增强含有活跃P-gp的初级AML爆发细胞对蒽环类抗生素（daunorubicin、idarubicin、mitoxantrone）和吉木替尼（Mylotarg）的细胞毒性。[2] 最新的研究表明，Zosuquidar完全抑制在ABCB1转导细胞中(Z)-endoxifen的顶向转运。[3]
体内活性	Zosuquidar trihydrochloride 在血脑屏障作为P-gp的抑制剂仅表现出适度活性。口服25 mg/kg的Zosuquidar trihydrochloride能在给予紫杉醇后1小时内使大脑浓度约增加2.5倍，在24小时后增加5倍。Zosuquidar 以剂量依赖的方式增强了奈非那韦进入大脑的吸收。在没有Zosuquidar给药的情况下，大脑组织/血浆中奈非那韦的浓度比为0.06±0.03，而在给予2 mg/kg静脉注射Zosuquidar后2至6小时之间增至0.09±0.02，6小时后达到0.85±0.19，20 mg/kg Zosuquidar后增至1.58±0.67。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 50 mg/mL (78.49 mM)
关键字	LY335979 Trihydrochloride \| CEM/VLB100 \| Pgp \| 2780AD \| Multidrug resistance protein 1 \| Zosuquidar \| CD243 \| Zosuquidar (LY335979) \| anti-tumor activity \| LY 335979 \| P388/ADR \| LY335979 \| P-glycoprotein \| UCLA-P3.003VLB \| 2780 \| RS 33295-198 (D06387) \| LY-335979 Trihydrochloride \| RS 33295-198 \| ABCB1 \| LY 335979 Trihydrochloride \| MCF7 \| acute myelogenous leukemia \| MDR1 \| HL60 \| P-gp \| UCLA-P3 \| Zosuquidar Trihydrochloride \| P388 \| MCF7/ADR \| RS 33295-198 Trihydrochloride \| CCRF-CEM \| K562 \| LY-335979 \| Inhibitor \| Zosuquidar trihydrochloride \| Cluster of differentiation 243 \| AML \| inhibit
相关产品	Elacridar \| Cinchonine \| Piperine \| P-gp inhibitor 1 \| Glibenclamide \| Atazanavir \| Selamectin \| Polyoxyethylene stearate \| Atazanavir sulfate \| Muscone \| Encequidar mesylate \| Verapamil

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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