[CAS NO. 211915-06-9] Dabigatran (BIBR-1048) etexilate

Name: Dabigatran (BIBR-1048) etexilate
Brand: Arctom Scientific
SKU: SLK-S2154

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PRODUCTS SPECIFICATIONS [211915-06-9]

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Catalog

SLK-S2154

Brand

Selleck

CAS

211915-06-9

DESCRIPTION [211915-06-9]

Overview

MDL	MFCD16038312
Molecular Weight	627.73
Molecular Formula	C34H41N7O5
SMILES	CN1C=2C(=CC(C(N(CCC(OCC)=O)C3=CC=CC=N3)=O)=CC2)N=C1CNC4=CC=C(C(NC(OCCCCCC)=O)=N)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.5930 mL	7.9652 mL	15.9304 mL
5 mM	0.3186 mL	1.5930 mL	3.1861 mL
10 mM	0.1593 mL	0.7965 mL	1.5930 mL
50 mM	0.0319 mL	0.1593 mL	0.3186 mL

Description

Dabigatran Etexilate (BIBR-1048) is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the molecule.

Targets

Thrombin ^[1]

In vitro

Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran inhibits thrombin generation in platelet-poor plasma (PPP) with IC50 of 0.56 μM, measured as the endogenous thrombin potential (ETP). Dabigatran demonstrates concentrationdependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 μM, respectively.

In vivo

Dabigatran prolongs the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dabigatran etexilate (20 mg/kg, orally) produces less prolongation of K value and less decreases in angle and maximum amplitude than enoxaparin in swine. Dabigatran (0.01-0.1 mg/kg) reduces thrombus formation dose-dependently, with an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. Dabigatran etexilate (5-30 mg/kg) inhibits thrombus formation in a dose- and time-dependent manner, with maximum inhibition within 30 min of pretreatment, suggesting a rapid onset of action.

References

[1] Wienen W, et al. Thromb Haemost, 2007, 98(1), 155-162.
[2] McKellar SH, et al. J Thorac Cardiovasc Surg, 2011, 141(6), 1410-1416.
[3] Wienen W, et al. Thromb Haemost, 2007, 98(2), 333-338.

Synonyms

β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl]amino]iminomethyl]phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-, ethyl ester

Dabigatran etexilate

BIBR 1048

Prazaxa