唑喹達三鹽酸鹽|T6018|TargetMol

價格	￥315	￥745	￥1070
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-24

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產(chǎn)品詳情

中文名稱:唑喹達三鹽酸鹽	英文名稱:Zosuquidar trihydrochloride
CAS:167465-36-3	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.55%	產(chǎn)品類別: 抑制劑
貨號: T6018

Product Introduction

Bioactivity

名稱	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.
細(xì)胞實驗	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)
激酶實驗	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.
體外活性	Zosuquidar通過阻斷[3H]azidopine光親和標(biāo)記CEM/VLB100質(zhì)膜中的Pgp，競爭性抑制[3H]vinblastine與Pgp的平衡結(jié)合。[1] Zosuquidar單獨對藥物敏感和多藥抗性（MDR）細(xì)胞系表現(xiàn)出具有IC50在6 μM至16 μM范圍內(nèi)的細(xì)胞毒性，并且能夠以0.1及0.5 μM濃度完全逆轉(zhuǎn)MDR細(xì)胞系P388/ADR、MCF7/ADR、2780AD或UCLA-P3.003VLB對化療化合物（vinblastine、doxorubicin或etoposide）的抗性。[1] Zosuquidar顯著恢復(fù)表達P-gp的白血病細(xì)胞系（包括K562/HHT40、K562/HHT90、K562/DOX和HL60/DNR）對藥物的敏感性，并增強含有活躍P-gp的初級AML爆發(fā)細(xì)胞對蒽環(huán)類抗生素（daunorubicin、idarubicin、mitoxantrone）和吉木替尼（Mylotarg）的細(xì)胞毒性。[2] 最新的研究表明，Zosuquidar完全抑制在ABCB1轉(zhuǎn)導(dǎo)細(xì)胞中(Z)-endoxifen的頂向轉(zhuǎn)運。[3]
體內(nèi)活性	Zosuquidar trihydrochloride 在血腦屏障作為P-gp的抑制劑僅表現(xiàn)出適度活性?？诜?5 mg/kg的Zosuquidar trihydrochloride能在給予紫杉醇后1小時內(nèi)使大腦濃度約增加2.5倍，在24小時后增加5倍。Zosuquidar 以劑量依賴的方式增強了奈非那韋進入大腦的吸收。在沒有Zosuquidar給藥的情況下，大腦組織/血漿中奈非那韋的濃度比為0.06±0.03，而在給予2 mg/kg靜脈注射Zosuquidar后2至6小時之間增至0.09±0.02，6小時后達到0.85±0.19，20 mg/kg Zosuquidar后增至1.58±0.67。
存儲條件	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)
關(guān)鍵字	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
相關(guān)產(chǎn)品	Elacridar \| Cinchonine \| P-gp inhibitor 1 \| Glibenclamide \| Verapamil hydrochloride \| Atazanavir \| Polyoxyethylene stearate \| Atazanavir sulfate \| Muscone \| Encequidar mesylate

關(guān)鍵字： Zosuquidar (LY335979) 3HCl|||唑喹達三鹽酸鹽|||RS 33295-198 trihydrochloride|||RS 33295-198 (D06387) 3HCl|||Zosuquidar 3HCl|||LY-335979 trihydrochloride|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個性化定制合成；從對明確靶點的分子篩選到對明確分子的多靶點篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國市場五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊資本	566.2651萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場三路28號4樓

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