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Dabigatran Etexilate Mesylate

Dabigatran Etexilate Mesylate
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Purity:99.94%
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Dabigatran Etexilate Mesylate

Catalog No. T5133Cas No. 872728-81-9
Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).
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Pack SizePriceAvailabilityQuantity
5 mg$35In Stock
10 mg$52In Stock
25 mg$68In Stock
50 mg$87In Stock
100 mg$113In Stock
200 mg$172In Stock
500 mg$253In Stock
1 mL x 10 mM (in DMSO)$58In Stock
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Product Introduction

Bioactivity
Description
Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).
In vitro
Dabigatran selectively and reversibly inhibited 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. Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC50: 0.56 μM). Dabigatran demonstrated concentration-dependent 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].
In vivo
Dabigatran prolonged 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). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial hemorrhages and hemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].
AliasBIBR 1048MS, Dabigatran etexilate methanesulfonate
Chemical Properties
Molecular Weight723.84
FormulaC34H41N7O5.CH4O3S
Cas No.872728-81-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 50 mg/mL (69.08 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.3815 mL6.9076 mL13.8152 mL69.0760 mL
5 mM0.2763 mL1.3815 mL2.7630 mL13.8152 mL
10 mM0.1382 mL0.6908 mL1.3815 mL6.9076 mL
20 mM0.0691 mL0.3454 mL0.6908 mL3.4538 mL
50 mM0.0276 mL0.1382 mL0.2763 mL1.3815 mL

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