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BIBR-1048

Catalog No.
A8381
Thrombin inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$77.00
In stock
5mg
$66.00
In stock
10mg
$92.00
In stock
50mg
$131.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Dabigatran etexilate is a potent, selective and competitive inhibitor of thrombin. It is an oral prodrug of dabigatran. Ki=4.5 nM for human thrombin and IC50=10 nM for thrombin-induced platelet aggregation. [1] [2]

Thrombin is protein that proteolytically cleaved from coagulation factor II as the initial step in the coagulation cascade. It transforms fibrinogen into fibrin and activates other factors in function in blood homeostasis, wound healing and inflammation.

In vitro, dabigatran showed anticoagulant effects in a concentration-dependent manner. It doubled the activated partrial thromboplastin time, prothrombin time and ecarin clotting in human PPP. [1]

In rats and rhesus monkeys, activated partial throboplastin time was extended by dabigaran.

Rats orally administrated with dabigatran etexilate exerted anticoagulant effects in a dose and time –dependent manner. [1]

Compared with warfarin, dabigatran administered orally (150 mg dose) in patients with atrial fibraillation, exhibited lower rates of stroke and systemic embolism but similar rates of major hemorrhage. [2]

References:
1.? Wienen W, Stassen JM, Priepke H et al. In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62.
2.? Connolly SJ, Ezekowitz MD, Yusuf S et al. Dabigatran versus warfarin in patients with atrial
fibrillation.? N Engl J Med. 2009 Sep 17;361(12):1139-51.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt627.73
Cas No.211915-06-9
FormulaC34H41N7O5
Solubility≥30 mg/mL in DMSO; insoluble in H2O; ≥22.13 mg/mL in EtOH
Chemical Nameethyl 3-[[2-[[4-[(Z)-N'-hexoxycarbonylcarbamimidoyl]anilino]methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoate
SDFDownload SDF
Canonical SMILESCCCCCCOC(=O)N=C(C1=CC=C(C=C1)NCC2=NC3=C(N2C)C=CC(=C3)C(=O)N(CCC(=O)OCC)C4=CC=CC=N4)N
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control