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

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Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP
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Solubility

In vitro
Batch:

DMSO : 9 mg/mL (17.69 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 9 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	508.63	Formula	C₂₃H₃₆N₆O₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	74863-84-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			SMILES	CC1CCN(C(C1)C(=O)O)C(=O)C(CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	Thrombin 5-39 nM(Ki)
In vitro	Argatroban (MCI-9038) is a potent and selective synthetic thrombin inhibitor with Ki values against thrombin ranging from 5 nM to 39 nM. It has antithrombotic properties in a wide variety of animal models of both platelet-rich and erythrocyte-rich thrombosis. This compound dose-dependently prevents thrombus formation with an estimated ED50 of 125 μg/kg in this test. It produces 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 (MCI-9038) inhibits the formation of microthrombi up to 3 hours after middle cerebral artery (MCA) occlusion; beyond 3 hours, it is ineffective. This compound also significantly reduces the size of ischemic cerebral lesions at 6 hours after MCA occlusion. At a dosage of 0.3 mg/h/rat, it 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. It (0.3 mg/h/rat) also significantly reduces the size of the cerebral infarction.
References	[1] https://pubmed.ncbi.nlm.nih.gov/7889274/ [2] https://pubmed.ncbi.nlm.nih.gov/12568910/ [3] https://pubmed.ncbi.nlm.nih.gov/8569051/ [4] https://pubmed.ncbi.nlm.nih.gov/8768731/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-04-02)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07499037	NOT_YET_RECRUITING	Pneumonia; Heart Failure	University Hospital Ostrava	2027-01	PHASE2
NCT06442267	RECRUITING	Respiratory Insufficiency; Circulatory Failure; Thromboembolism; Bleeding	Medical University of Vienna	2024-07-30	PHASE4
NCT05226442	COMPLETED	Extracorporeal Membrane Oxygenation Complication; Anticoagulants and Bleeding Disorders	Medical University of Vienna	2021-12-01	PHASE2; PHASE3
NCT04925167	COMPLETED	Respiratory Failure	Beijing Chao Yang Hospital	2021-07-06
NCT03735979	COMPLETED	Acute Ischemic Stroke	Washington University School of Medicine	2019-10-15	PHASE3
NCT06066762	Not yet recruiting	Heparin-induced Thrombocytopenia	Assistance Publique - Hôpitaux de Paris	2023-11-01	--

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Argatroban (MCI-9038) Thrombin inhibitor

Chemical Structure

Molecular Weight: 508.63