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Argatroban (MCI-9038) Thrombin inhibitor

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

Cat.No.S2069

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

Chemical Structure

Molecular Weight: 508.63

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.94%

99.94

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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

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
=	×	×

Dilution Calculator Molecular Weight Calculator

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.

Mechanism of Action

Targets/IC₅₀/Ki	Thrombin ^[1] 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. ^[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 (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. ^[3] 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. ^[4]
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 2024-05-22)

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

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