Dabigatran etexilate mesylate - CAS 872728-81-9
Catalog number: 872728-81-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C35H45N7O8S
Molecular Weight:
723.84
COA:
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Targets:
Thrombin
Description:
Dabigatran etexilate mesylate is the orally active prodrug of dabigatran. It is a reversible and selective, direct thrombin inhibitor (DTI).
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Purity:
>98%
Related CAS:
872728-81-9 (Dabigatran etexilate mesylate); 211915-06-9 (Dabigatran etexilate); 211914-51-1 (Dabigatran)
Appearance:
Solid powder
Synonyms:
Ethyl 3-(((2-(((4-(((hexyloxy)carbonyl)carbamimidoyl)phenyl)amino)methyl)-1-methyl-1h-benzimidazol-5-yl)carbonyl)(pyridin-2-yl)amino)propanoate, methanesulfonate; Dabigatran etexilate mesylate; BIBR 1048MS; BIBR1048MS; BIBR-1048MS; BIBR 1048; BIBR1048; BIBR-1048; band name: Pradaxa
MSDS:
Inquire
InChIKey:
XETBXHPXHHOLOE-UHFFFAOYSA-N
InChI:
1S/C34H41N7O5.CH4O3S/c1-4-6-7-10-21-46-34(44)39-32(35)24-12-15-26(16-13-24)37-23-30-38-27-22-25(14-17-28(27)40(30)3)33(43)41(20-18-31(42)45-5-2)29-11-8-9-19-36-29;1-5(2,3)4/h8-9,11-17,19,22,37H,4-7,10,18,20-21,23H2,1-3H3,(H2,35,39,44);1H3,(H,2,3,4)
Canonical 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
1.Expression of pro-inflammatory genes in human endothelial cells: Comparison of rivaroxaban and dabigatran.
Ellinghaus P1, Perzborn E2, Hauenschild P3, Gerdes C4, Heitmeier S5, Visser M6, Summer H7, Laux V8. Thromb Res. 2016 Apr 16;142:44-51. doi: 10.1016/j.thromres.2016.04.008. [Epub ahead of print]
INTRODUCTION: In addition to its central role in coagulation, thrombin is involved in non-hemostatic activities such as inflammation. Direct inhibition of thrombin activity (e.g. with dabigatran) or reducing its generation by inhibition of Factor Xa (e.g. with rivaroxaban) may therefore have anti-inflammatory effects.
2.Net Clinical Benefit of Dabigatran Over Warfarin in Patients With Atrial Fibrillation Stratified by CHA2DS2-VASc and Time in Therapeutic Range.
Chan PH1, Huang D1, Lau CP1, Chan EW2, Wong IC2, Lip GY3, Tse HF1, Siu CW4. Can J Cardiol. 2016 Jan 25. pii: S0828-282X(16)00056-8. doi: 10.1016/j.cjca.2016.01.016. [Epub ahead of print]
BACKGROUND: Although dabigatran is 1 of the preferred agents for stroke prevention in atrial fibrillation, warfarin remains the mainstay treatment in many publicly financed health care systems. Little is known about the net clinical benefit of switching patients who are receiving warfarin and have different risk profiles and time in therapeutic range (TTR) to dabigatran. In this study, we aimed to investigate the net clinical benefit of switching warfarin to dabigatran in relation to CHA2DS2-VASc and TTR.
3.Efficacy of prothrombin complex concentrates for the emergency reversal of dabigatran-induced anticoagulation.
Grottke O1, Aisenberg J2, Bernstein R3, Goldstein P4, Huisman MV5, Jamieson DG6, Levy JH7, Pollack CV Jr8, Spyropoulos AC9, Steiner T10, Del Zoppo GJ11, Eikelboom J12. Crit Care. 2016 Apr 28;20(1):115. doi: 10.1186/s13054-016-1275-8.
Dabigatran is effective in decreasing the risk of ischaemic stroke in patients with atrial fibrillation. However, like all anticoagulants, it is associated with a risk of bleeding. In cases of trauma or emergency surgery, emergency reversal of dabigatran-induced anticoagulation may be required. A specific reversal agent for dabigatran, idarucizumab, has been approved by the US Food and Drug Administration. Alternative reversal agents are available, such as prothrombin complex concentrates (PCCs) and activated PCCs (aPCCs). In this review we evaluate the role of PCCs and aPCCs in the reversal of dabigatran anticoagulation and consider which tests are appropriate for monitoring coagulation in this setting. Pre-clinical studies, small clinical studies and case reports indicate that PCCs and aPCCs may be able to reverse dabigatran-induced anticoagulation in a dose-dependent manner. However, dosing based on coagulation parameters can be difficult because available assays may not provide adequate sensitivity and specificity for measuring anticoagulation induced by dabigatran or the countering effects of PCCs/aPCCs.
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CAS 872728-81-9 Dabigatran etexilate mesylate

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