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Dabigatran etexilate mesylate

CAS No. 872728-81-9

Dabigatran etexilate mesylate( BIBR 1048MS | Dabigatran etexilate methanesulfonate )

Catalog No. M16346 CAS No. 872728-81-9

A prodrug of BIBR-953, which is a potent nonpeptide thrombin inhibitor with Ki of 4.5 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 36 In Stock
5MG 36 In Stock
10MG 51 In Stock
25MG 66 In Stock
50MG 78 In Stock
100MG 105 In Stock
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Biological Information

  • Product Name
    Dabigatran etexilate mesylate
  • Note
    Research use only, not for human use.
  • Brief Description
    A prodrug of BIBR-953, which is a potent nonpeptide thrombin inhibitor with Ki of 4.5 nM.
  • 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.
  • In Vitro
    ——
  • 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.
  • Synonyms
    BIBR 1048MS | Dabigatran etexilate methanesulfonate
  • Pathway
    Autophagy
  • Target
    Thrombin
  • Recptor
    Thrombin-inducedplateletaggregation
  • Research Area
    Cardiovascular Disease
  • Indication
    Thrombosis

Chemical Information

  • CAS Number
    872728-81-9
  • Formula Weight
    723.8389
  • Molecular Formula
    C35H45N7O8S
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • 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
  • Chemical Name
    β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl]amino]iminomethyl]phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-, ethyl ester, methanesulfonate (1:1)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Hauel NH, et al. J Med Chem. 2002 Apr 25;45(9):1757-66. 2. Wienen W, et al. Thromb Haemost. 2007 Jul;98(1):155-62. 3. Baetz BE, et al. Pharmacotherapy. 2008 Nov;28(11):1354-73.
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  • Dabigatran etexilate...

    A prodrug of BIBR-953, which is a potent nonpeptide thrombin inhibitor with Ki of 4.5 nM.