Dabigatran etexilate mesylate

SKU: orb1223784

Description

A prodrug of BIBR-953, which is a potent nonpeptide thrombin inhibitor with Ki of 4.5 nM; 10-fold less potent for Trypsin and no activity against Factor Xa, Plasmin, tPA and activated protein C; exhibits strong and long-lasting anticoagulant effects ex vivo and strong oral activity in different animal species.Thrombosis Approved(In Vivo):Dabigatran etexilate mesylate (BIBR 1048MS; oral; 10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys) has dose- and time-dependent anticoagulant effects and has maximum effects between 30 and 120 min after administration, respectively.Dabigatran etexilate mesylate maximally and significantly prolongs partial thromboplastin time (aPTT) to 25.2, 38.4 and 78.3 s in 30 min after 10, 20 and 50 mg/kg oral doses, respectively.Dabigatran etexilate mesylate maximally prolongs the aPTT to 34.3 s, 44.0 s, and 63.0 s, respectively, 2h after 1, 2.5 or 5 mg/kg doses in the monkey.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 872728-81-9
• MW: 723.8389
• Purity: >98% (HPLC)
• Formula: C₃₅H₄₅N₇O₈S
• SMILES: O=C(OCC)CCN(C(C1=CC=C2C(N=C(CNC3=CC=C(C(NC(OCCCCCC)=O)=N)C=C3)N2C)=C1)=O)C4=NC=CC=C4.CS(=O)(O)=O
• Target: Thrombin
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Dabigatran etexilate mesylate (BIBR 1048MS; oral; 10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys) has dose-and time-dependent anticoagulant effects and has maximum effects between 30 and 120 min after administration, respectively. Dabigatran etexilate mesylate maximally and significantly prolongs partial thromboplastin time (aPTT) to 25.2, 38.4 and 78.3 s in 30 min after 10, 20 and 50 mg/kg oral doses, respectively. Dabigatran etexilate mesylate maximally prolongs the aPTT to 34.3 s, 44.0 s, and 63.0 s, respectively, 2h after 1, 2.5 or 5 mg/kg doses in the monkey. Animal model: Male rats (280-350 g) and rhesus monkeys of either sex (3-8 kg). Dosage: 10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys. Administration: Oral. Result: Had dose-and time-dependent anticoagulant effects.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BIBR 1048MS | Dabigatran etexilate methanesulfonate

Quick Database Links

Gene Symbol

Thrombin