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Argatroban (MCI-9038)

Name: Argatroban (MCI-9038)
Brand: Selleck Chemicals
SKU: S2069
Rating: 5 (7 reviews)

Catalog No.S2069 Purity:99.94%

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

Argatroban (MCI-9038) Chemical Structure

CAS No. 74863-84-6

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 K_i 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

[4] Kawai H, et al. J Pharmacol Exp Ther,?996, 278(2), 780-785.

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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