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Argatroban Monohydrate Thrombin inhibitor

Name: Argatroban Monohydrate
Brand: Selleck Chemicals
SKU: S5074
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S5074

Argatroban (Argatroban hydrate, Argipidine,MCI-9038 Monohydrate) is a direct, selective thrombin inhibitor with anticoagulant effects.

Chemical Structure

Molecular Weight: 526.65

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

Quality Control

Batch: S507401 DMSO]100 mg/mL]false]Ethanol]40 mg/mL]false]Water]Insoluble]false Purity: 99.99%

99.99

Related Targets	HDAC Caspase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease Proteasome Serine Protease Secretase PCSK9 Glutaminase Acyltransferase Cathepsin B MALT PAD PREP Neprilysin SGK Aminopeptidase 3C-Like Protease PGDS GOT

Chemical Information, Storage & Stability

Molecular Weight	526.65	Formula	C₂₃H₃₆N₆O₅S.H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	141396-28-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Argatroban hydrate, Argipidine,MCI-9038 Monohydrate			Smiles	CC1CCN(C(C1)C(=O)O)C(=O)C(CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C.O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (189.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 40 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.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.250mg/ml (4.27mM)	Taking the 1 mL working solution as an example, add 50 μL of 45 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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]
In vitro	Argatroban is highly selective for thrombin and has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein). Argatroban is effective against free, fibrin-bound and clot-bound thrombin with comparable half-maximal inhibitory concentrations (IC50), and argatroban is also effective in inhibiting platelet aggregation and thromboxane generation in the presence of both free and clot-bound thrombin^[1]. Argatroban binds thrombin and inhibits its activity without the requirement of coenzymes, unlike antithrombin III or heparin cofactor II. Argatroban decreases bone metastasis of B16 mouse melanoma cells by inactivating thrombin activity. Moreover, argatroban has potential to inhibit PAR-2 activation by interfering with the thrombogenic cycle. It does not have toxic effect for tumor cells^[2].
In vivo	Within a clinically relevant dose range (from 1–3 μg/kg/min in prevention or treatment of thrombotic events in HIT to up to 25 μg/kg/min in PCI in HIT patients), argatroban exhibits linear pharmacokinetic behavior, and steady state levels are attained within 1 hour after the start of an infusion. The elimination half-life of argatroban in healthy subjects is about 45 minutes, with a corresponding decline in its anticoagulant effects which reach their pretreatment level within 2–4 hours after cessation of an infusion. Argatroban lacks major drug–drug interactions with CYP3A4/5 inhibitors such as erythromycin or with acetaminophen, warfarin, and digoxin. However, in patients with hepatic impairment, area under the concentration versus time curve (AUC), maximum concentration, and half-life of argatroban were increased approximately 2- to 3-fold, and clearance was one-fourth that of healthy volunteers. The increase in plasma concentrations in these patients coincided with increased pharmacodynamic effects^[1].
References	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2721302/ https://pubmed.ncbi.nlm.nih.gov/22359194/

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