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Dabigatran etexilate mesylate

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Dabigatran etexilate mesylate
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Cat #: V12492 CAS #: 872728-81-9 Purity ≥ 98%

Description: Dabigatran Etexilate mesylate (BIBR-1048; BIBR 1048MS) is the prodrug of dabigatran which is a potent and nonpeptidic small molecule anti-thrombotic agent that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.

References: Wienen W, et al. In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally activeprodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62.

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Molecular Weight (MW)C35H45N7O8S
Molecular Formula723.84
CAS No.872728-81-9
SMILES CodeO=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           
SynonymsDabigatran etexilate mesylate; BIBR 1048MS; BIBR1048MS; BIBR-1048MS; BIBR 1048; BIBR1048; BIBR-1048; band name: Pradaxa.
ProtocolIn VivoDabigatran 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. 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 (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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Quality Control Documentation
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Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.