.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 627,73 Дабигатран этексилат - это пролекарство дабигатрана, мощной, непептидной небольшой молекулы, которая специфически и обратимо ингибирует как свободный, так и связанный со сгустком тромбин, связываясь с активным сайтом молекула тромбина. \ n Биологическая активность
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Description
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Dabigatran Etexilate is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.
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In vitro
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Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran inhibits thrombin generation in platelet-poor plasma (PPP) with IC50 of 0.56 μM, measured as the endogenous thrombin potential (ETP). Dabigatran demonstrates concentrationdependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 μM, respectively. [1]
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In vivo
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Dabigatran prolongs the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). [1] Dabigatran etexilate (20 mg/kg, orally) produces less prolongation of K value and less decreases in angle and maximum amplitude than enoxaparin in swine. [2] Dabigatran (0.01-0.1 mg/kg) reduces thrombus formation dose-dependently, with an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. Dabigatran etexilate (5-30 mg/kg) inhibits thrombus formation in a dose- and time-dependent manner, with maximum inhibition within 30 min of pretreatment, suggesting a rapid onset of action.[3]
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Features
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Протокол (только для справки) Конверсия различных модельных животных на основе BSA (значение на основе данных из проекта руководящих принципов 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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1 Ссылки [1] Wienen W, et al. Тромб Хемост, 2007, 98 (1), 155-162. [2] McKellar SH, et al. J Thorac Cardiovasc Surg, 2011, 141 (6), 1410-1416. [3] Wienen W, et al. Тромб Хемост, 2007, 98 (2), 333-338. \ n Химическая информация
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Molecular Weight (MW)
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627.73
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Formula
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C34H41N7O5
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CAS No.
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211915-06-9
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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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BIBR-1048
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Solubility (25°C) *
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In vitro
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DMSO
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126 mg/mL
(200.72 mM)
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Water
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<1 mg/mL
(
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Ethanol
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12 mg/mL
(19.11 mM)
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Chemical Name
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(E)-ethyl 3-(2-((4-(N'-(hexyloxycarbonyl)carbamimidoyl)phenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoate
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Stock Solution (1ml DMSO)
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1mM
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10mM
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20mM
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30mM
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Mass(mg)
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0.62773
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6.2773
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12.5546
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18.8319
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Группа Продуктов : Другие > Ингибитор тромбина
