Catalog No.S2069 Synonyms: MCI-9038
Molecular Weight(MW): 508.63
Argatroban is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM, used as an anticoagulant.
Purity & Quality Control
Choose Selective Thrombin Inhibitors
|Description||Argatroban is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM, used as an anticoagulant.|
Argatroban is a potent and selective synthetic thrombin inhibitor with Ki values against thrombin ranging from 5 nM to 39 nM. Argatroban has antithrombotic properties in a wide variety of animal models of both platelet-rich and erythrocyte-rich thrombosis. Argatroban dose-dependently prevents thrombus formation with an estimated ED50 of 125 μg/kg in this test. Argatroban produces a dose-dependent increases in the thrombin time with a 511% increase at the highest dose used with only a 73% increase in the APTT at this dose.  Argatroban can directly induce phenotype conversion of vascular smooth muscle cells with the resultant up-regulation of SMemb, PAI-1, and beta-actin mRNAs. 
|In vivo||Argatroban inhibits the formation of microthrombi up to 3 hours after middle cerebral artery (MCA) occlusion; beyond 3 hours, it is ineffective. Argatroban also significantly reduces the size of ischemic cerebral lesions at 6 hours after MCA occlusion.  Argatroban (0.3 mg/h/rat) significantly decreases the number of microthrombi 1 day after distal middle cerebral artery (dMCA) occlusion in the rat distal middle cerebral artery occlusion model. Argatroban (0.1 and 0.3 mg/h/rat) significantly reverses a decrease in regional cerebral blood flow (rCBF) 1 day after distal middle cerebral artery (dMCA) occlusion. Argatroban (0.3 mg/h/rat) also significantly reduces the size of the cerebral infarction. |
|In vitro||DMSO||9 mg/mL (17.69 mM)|
|Ethanol||6 mg/mL (11.79 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02935530||Recruiting||Gynecologic Neoplasms|Venous Thromboembolism|Low Molecular Weight Heparin|Argatroban||Huazhong University of Science and Technology||January 2016||Phase 3|
|NCT02448069||Recruiting||Stroke|Cerebral Ischemia||The University of Texas Health Science Center, Houston||May 2015||Phase 2|
|NCT01734252||Recruiting||Achievement of a Sufficient Thrombosis Prohpylaxis in Clitically Ill Patients With Heparin Resistance||Medical University Innsbruck||June 2012||Phase 2|
|NCT01464788||Terminated||Ischemic Stroke||Andrew D. Barreto, MD|The University of Texas Health Science Center, Houston||October 2011||Phase 2|
|NCT01246011||Terminated||Coronary Artery Bypass Graft Surgery|Presence of Heparin/Platelet Factor 4 Antibody||Massachusetts General Hospital|GlaxoSmithKline||November 2010||Phase 4|
|NCT01163604||Completed||CVD||Jinling Hospital, China||August 2010||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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