Dabigatran Etexilate - CAS 211915-06-9
Catalog number:
211915-06-9
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Thrombin
Description:
Dabigatran etexilate(BIBR-1048) is the orally active prodrug of dabigatran; Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.
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Purity:
0.99
Synonyms:
Prazaxa; BIBR 1048; BIBR-1048
MSDS:
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1.Laboratory determination of old and new targeted anticoagulant agents for prevention of bleeding and thrombotic events in cancer patients.
Harenberg J1. Thromb Res. 2016 Apr;140 Suppl 1:S165-7. doi: 10.1016/S0049-3848(16)30117-7.
A two-fold prolongation of activated partial thromboplastin time (APTT) is established as therapeutic range for therapy with unfractionated heparin, hirudin and argatroban. The international normalized ratio (INR) of 2 to 3 is required to maintain anticoagulation in the therapeutic range of vitamin K antagonists. The therapeutic range of anti-factor Xa activity during therapy with low-molecular weight heparins and danaparoid are less well and of direct oral anticoagulants (DOAC) poorly defined. The relation of aPTT and INR values to thrombotic and bleeding events are well established despite a large variation of values in affected patients. The relation of coagulation values of the other anticoagulants to clinical events is open. The value of determination in cancer patients is higher because of the increased risk for thrombotic and bleeding events of this patient group. Several activities are currently undertaken to certify methods for in vitro diagnostic testing for DAOCs.
2.Who Were the Early Adopters of Dabigatran?: An Application of Group-based Trajectory Models.
Lo-Ciganic WH1, Gellad WF, Huskamp HA, Choudhry NK, Chang CH, Zhang R, Jones BL, Guclu H, Richards-Shubik S, Donohue JM. Med Care. 2016 Apr 25. [Epub ahead of print]
BACKGROUND: Variation in physician adoption of new medications is poorly understood. Traditional approaches (eg, measuring time to first prescription) may mask substantial heterogeneity in technology adoption.
3.Post-marketing surveillance on the long-term use of dabigatran in Japanese patients with nonvalvular atrial fibrillation: Preliminary report of the J-dabigatran surveillance.
Inoue H1, Uchiyama S2, Atarashi H3, Okumura K4, Koretsune Y5, Yasaka M6, Yamashita T7, Ohnishi M8, Yagi N9, Fukaya T10; J-Dabigatran Surveillance Investigators. J Arrhythm. 2016 Apr;32(2):145-50. doi: 10.1016/j.joa.2015.11.008. Epub 2016 Jan 16.
BACKGROUND/AIM: A post-marketing surveillance (PMS) study is being conducted to investigate the safety and effectiveness of the long-term use of dabigatran etexilate (dabigatran) in Japanese patients with nonvalvular atrial fibrillation (NVAF). Results of an interim analysis of this prospective cohort study including patient characteristics and adverse drug reactions (ADRs) collected up to September 17, 2014 are reported here.
4.Hypercoagulability causes atrial fibrosis and promotes atrial fibrillation.
Spronk HM1, De Jong AM2, Verheule S3, De Boer HC4, Maass AH2, Lau DH3, Rienstra M2, van Hunnik A3, Kuiper M3, Lumeij S3, Zeemering S3, Linz D5, Kamphuisen PW6, Ten Cate H1, Crijns HJ7, Van Gelder IC2, van Zonneveld AJ4, Schotten U8. Eur Heart J. 2016 Apr 12. pii: ehw119. [Epub ahead of print]
AIMS: Atrial fibrillation (AF) produces a hypercoagulable state. Stimulation of protease-activated receptors by coagulation factors provokes pro-fibrotic, pro-hypertrophic, and pro-inflammatory responses in a variety of tissues. We studied the effects of thrombin on atrial fibroblasts and tested the hypothesis that hypercoagulability contributes to the development of a substrate for AF.
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