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BIBR 953 (Dabigatran, Pradaxa)
Cat No.
CEI-1243
Description
BIBR 953 is a potent nonpeptide inhibitor of thrombin with IC50 value of 9.3 nM.
Product Overview
BIBR 953 is a potent, reversible, and direct inhibitor of thrombin with IC50 value of 9.3nM. BIBR 953 shows a favorable selectivity profile and strong activity in vitro with a Ki value of 4.5nM. It also exhibits the best activity profile in vivo following administration to rats. BIBR 953 is designed to be converted into an orally active prodrug BIBR 1048 due to its highly polar, zwitterionic nature and poor oral absorption. BIBR 953 inhibits thrombin in a competitive fashion. This inhibition is rapid and reversible. BIBR 953 inhibits both clot-bound and free thrombin. BIBR 953 is demonstrated to have an anticoagulant efficacy both in vitro and ex vivo. Since thrombin can affect cell behavior and response in various tissue types via PAR signaling, BIBR 953 is found to be beneficial in many diseases including inflammation, infection, fibrosis and cancer. Clinical trials show that BIBR 953 is a highly effective anticoagulant with a good safety profile.
CAS No.
211914-51-1
Molecular Weight
471.5
Purity
0.98
Storage
Store at -20°C
Targets
Thrombin
IC50
9.3 nM
Molecular Formula
C25H25N7O3
Chemical Name
3-[[2-[(4-carbamimidoylanilino)methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoic acid
Solubility
Limited solubility
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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