Dabigatran Etexilate Mesylate

SKU: orb1302061

Description

Dabigatran Etexilate Mesylate is an orally bioavailable prodrug that is rapidly converted to dabigatran, a potent, selective, and reversible direct thrombin inhibitor (Ki = 4.5 nM). It is widely used in research to study anticoagulation mechanisms and efficacy in both in vitro biochemical assays and in vivo thrombosis models.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 872728-81-9
• MW: 723.84
• Purity: 99.94% (May vary between batches)
• Formula: C₃₄H₄₁N₇O₅.CH₄O₃S
• SMILES: CS(O)(=O)=O.CCCCCCOC(=O)NC(=N)c1ccc(NCc2nc3cc(ccc3n2C)C(=O)N(CCC(=O)OCC)c2ccccn2)cc1
• Target: Thrombin
• Solubility: DMSO:245 mg/mL (338.47 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.76 mM)

Bioactivity

• Target IC50:
  Thrombin-induced platelet aggregation:10 nM|Thrombin-induced platelet aggregation:4.5 nM (Ki)
• 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 . 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 .
• 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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BIBR 1048MS, antithrombotic, anticoagulant, atrial, active, agent, Dabigatran etexilate, Dabigatran Etexilate Mesylate, Dabigatran etexilate methanesulfonate, Dabigatran, inhibit, orally, fibrillation, effects, Inhibitor, venousthromboembolism, prodrug, Thrombin

Compound Identifiers

PubChem CID

135566083