1. Metabolic Enzyme/Protease
  2. Thrombin
  3. Dabigatran etexilate mesylate

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

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

Dabigatran etexilate mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 108 In-stock
Estimated Time of Arrival: December 31
100 mg USD 144 In-stock
Estimated Time of Arrival: December 31
200 mg USD 216 In-stock
Estimated Time of Arrival: December 31
500 mg USD 312 In-stock
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1 g USD 432 In-stock
Estimated Time of Arrival: December 31
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10 g   Get quote  

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Description

Dabigatran etexilate mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM. IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1] in vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 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 (IC(50): 0.56 microM). 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 microM, 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 haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2]. Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1

Clinical Trial
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    90% corn oil

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

  • 2.

    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

  • 3.

    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

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

Purity: 99.60%

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Product Name:
Dabigatran etexilate mesylate
Cat. No.:
HY-10274A
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Dabigatran etexilate mesylate

Cat. No.: HY-10274A