Home Proteases Thrombin inhibitor Argatroban (MCI-9038) For research use only.

Argatroban (MCI-9038)

Argatroban (MCI-9038) is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM, used as an anticoagulant.

Argatroban (MCI-9038) Chemical Structure

Argatroban (MCI-9038) Chemical Structure

CAS: 74863-84-6

Selleck's Argatroban (MCI-9038) has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.94%
99.94

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Biological Activity

Description Argatroban (MCI-9038) 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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06066762 Not yet recruiting Heparin-induced Thrombocytopenia Assistance Publique - Hôpitaux de Paris November 1 2023 --
NCT05325346 Completed Heparin-induced Thrombocytopenia Veralox Therapeutics|Celerion March 7 2022 Phase 1
NCT05226442 Recruiting Extracorporeal Membrane Oxygenation Complication|Anticoagulants and Bleeding Disorders Medical University of Vienna December 1 2021 Phase 2|Phase 3
NCT04751357 Unknown status Heparin-induced Thrombocytopenia Medical University of Vienna August 1 2020 --
NCT06038682 Completed ARDS|COVID-19 University Hospital Ostrava April 1 2020 --
NCT02448069 Completed Stroke|Cerebral Ischemia The University of Texas Health Science Center Houston May 2015 Phase 2

Chemical lnformation & Solubility

Molecular Weight 508.63 Formula

C23H36N6O5S
CAS No. 74863-84-6 SDF Download Argatroban (MCI-9038) SDF
Smiles CC1CCN(C(C1)C(=O)O)C(=O)C(CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 9 mg/mL ( (17.69 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 9 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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