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Dabigatran etexilate mesylate (Synonyms: BIBR 1048MS; Dabigatran etexilate methanesulfonate)

Cat. No.: HY-10274A Purity: 99.60%
Handling Instructions

Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.

For research use only. We do not sell to patients.

Dabigatran etexilate mesylate Chemical Structure

Dabigatran etexilate mesylate Chemical Structure

CAS No. : 872728-81-9

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Based on 2 publication(s) in Google Scholar

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Description

Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation[1].

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[1].
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[1].
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[1].

Animal Model: Male rats (280-350 g) and rhesus monkeys of either sex (3-8 kg)[1]
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.
Clinical Trial
Molecular Weight

723.84

Formula

C₃₅H₄₅N₇O₈S

CAS No.

872728-81-9

SMILES

O=C(N(C1=NC=CC=C1)CCC(OCC)=O)C2=CC=C3C(N=C(N3C)CNC4=CC=C(C(NC(OCCCCCC)=O)=N)C=C4)=C2.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (69.08 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3815 mL 6.9076 mL 13.8152 mL
5 mM 0.2763 mL 1.3815 mL 2.7630 mL
10 mM 0.1382 mL 0.6908 mL 1.3815 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.45 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.45 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.45 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.60%

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Keywords:

Dabigatran etexilateBIBR 1048MSOthersantithromboticagentorallyactiveprodrugDabigatrananticoagulanteffectsvenousthromboembolismatrialfibrillationInhibitorinhibitorinhibit

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Dabigatran etexilate mesylate
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