Argatroban

Catalog No.S2069 Synonyms: MCI-9038

Argatroban Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 90 In stock
USD 270 In stock
USD 570 In stock
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Biological Activity

Description Argatroban is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM, used as an anticoagulant.
Targets
Thrombin [1]
5-39 nM(Ki)
In vitro

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. [1] Argatroban can directly induce phenotype conversion of vascular smooth muscle cells with the resultant up-regulation of SMemb, PAI-1, and beta-actin mRNAs. [2]

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. [3] 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. [4]

Protocol

Solubility (25°C)

In vitro DMSO 9 mg/mL (17.69 mM)
Ethanol 6 mg/mL (11.79 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 508.63
Formula

C23H36N6O5S

CAS No. 74863-84-6
Storage powder
Synonyms MCI-9038

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID