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 No. 74863-84-6

Purity & Quality Control

Argatroban (MCI-9038) Related Products

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 Information & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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