.cp_wz table {border-top: твердое тело 1px #ccc; border-left: твердое тело 1px #ccc; } .cp_wz таблица td {border-right: 1px solid #ccc; нижняя граница: сплошной 1px #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} \ n Молекулярный вес: \ n 327,12 Никлозамид может ингибировать репликацию ДНК и ингибировать STAT с IC50 0,7 мкМ. \ n Биологическая активность Никлозамид (никлозамид способен ингибировать репликацию SARS-CoV при микромолярной концентрации в Клетки Vero E6, инфицированные SARS-CoV. Никлозамид (Никлозамид ингибирует TNF-индуцированную репортерную активность NF-κB в зависимости от дозы и времени в клетках U2OS. Никлозамид (125 нМ) ингибирует активацию NF-κB, индуцированную p65, IKKα , IKKβ, IKKγ и TAK1 в клетках U2OS. Никлозамид (40 мг / кг / сут, внутрибрюшинно) ингибирует рост ксенотрансплантатов клеток AML у голых мышей, несущих опухоли ксенотрансплантата HL-60. Протокол (только для справки) Киназный анализ: [1]
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Protein Kinase profiling assay
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Assay for 22 different proteins kinases is carried out by ProQinase Gmbh. All of the protein kinases are expressed either in Sf9 insect cells or in E.coli as recombinant GST-fusion proteins or His-tagged proteins. Protein kinases are purified by affinity chromatography using either GSH-agarose or Ni_NTH-agarose. A radiometric protein kinase assay is used for measuring the kinase activity of the 22 protein kinases. Briefly, for each protein kinase, 50 μL reaction cocktail containing 60 mM HEPES-NaOH, 3 mM MgCl2, 3 mM MnCl2, 3 μM Na-orthovanadate, 1.2 mM DTT, 50 μg/mL PEG20000, 1 μM [γ-33P]-ATP, Niclosamide, adequate amount of enzyme and its substrate. The PKC-alpha assay additionally contain 1 mM Cacl2, 4 mM EDTA, 5 μg/mL phosphatidylserine and 1 μg/mL 1, 2-Dioleyl-glycerol. The reaction cocktails are incubated at 37 °C for 60 minutes and stop with 50 μL 2% (v/v) H3PO4. Incorporation of 33Pi is determined with a microplate scintillation counter. The activities and the IC50 values are calculated using Quattro Workflow V2.28.
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Клеточный анализ: [1]
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Cell lines
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Hela, A549, Du145, HT-29, A431, PC3 cells
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Concentrations
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16 μM
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Incubation Time
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72 hours
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Method
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Cells are plated in 96-well culture plates with cell density of 3-4 × 103 cells/well and treat with Niclosamide by adding 100 μL medium containing Niclosamide of various concentrations on the second day. After 72-hour's treatment, MTT is added to each well and incubated for additional 4-5 hours, and the absorbance is measured on a microplate reader at 570nm. Cell growth inhibition is evaluated as the ratio of the absorbance of the sample to that of the control. The results are representative of at least 3 independent experiments.
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Исследование на животных: [4]
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Animal Models
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nude mice bearing HL-60 xenograft tumors.
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Formulation
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DMSO
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Dosages
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40 mg/kg
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Administration
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Intraperitoneal injection
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Solubility
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1% DMSO/30% polyethylene glycol/1% Tween 80,
30 mg/mL
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* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Конверсия различных модельных животных на основе BSA (значение на основе данных из проекта рекомендаций FDA)
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Species
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Baboon
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Dog
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Monkey
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Rabbit
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Guinea pig
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Rat
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Hamster
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Mouse
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Weight (kg)
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12
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10
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3
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1.8
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0.4
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0.15
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0.08
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0.02
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Body Surface Area (m2)
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0.6
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0.5
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0.24
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0.15
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0.05
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0.025
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0.02
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0.007
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Km factor
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20
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20
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12
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12
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8
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6
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5
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3
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Animal A (mg/kg) = Animal B (mg/kg) multiplied by
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Animal B Km
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Animal A Km
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Например, чтобы изменить дозу ресвератрола, используемую для мыши (22,4 мг / кг), на дозу, основанную на BSA для крысы, умножьте 22,4 мг / кг на коэффициент Km для мыши, а затем разделите на коэффициент Km для крыса. Этот расчет дает эквивалентную дозу ресвератрола для крыс 11,2 мг / кг.
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Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
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mouse Km(3)
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= 11.2 mg/kg
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rat Km(6)
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Химическая информация
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Molecular Weight (MW)
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327.12
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Formula
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C13H8Cl2N2O4
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CAS No.
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50-65-7
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Storage
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3 years -20℃Powder
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6 months-80℃in solvent (DMSO, water, etc.)
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Synonyms
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Niclocide
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Solubility (25°C) *
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In vitro
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DMSO
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<1 mg/mL
(
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Water
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<1 mg/mL
(
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Ethanol
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<1 mg/mL
(
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In vivo
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1% DMSO/30% polyethylene glycol/1% Tween 80
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30 mg/mL
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* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Chemical Name
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Benzamide, 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy-
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Калькулятор молярности Калькулятор разведения Калькулятор молекулярной массы
Группа Продуктов : JAK / STAT > Ингибитор STAT
