Argatroban Monohydrate

Catalog No.S5074 Synonyms: Argatroban hydrate, Argipidine

For research use only.

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

Argatroban Monohydrate Chemical Structure

CAS No. 141396-28-3

Selleck's Argatroban Monohydrate has been cited by 1 Publication

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Biological Activity

Description Argatroban (Argatroban hydrate, Argipidine) is a direct, selective thrombin inhibitor with anticoagulant effects.
Targets
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].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: MDA-231 breast cancer cells
  • Concentrations: 0.1-1 μM
  • Incubation Time: 4 h
  • Method:

    Tissue factor (TF) activity was measured as factor X (FX) activation by the factor VIIa (FVIIa)/TF complex on MDA-231 cells. MDA-231 cells were starved in serum-free medium for 24 h, following incubation with FBS for 24 h (24-well plate, 2.0 × 105 cells/well). After starvation, MDA-231 cells were treated with thrombin (0.1-10 U/ml) in presence or absence of argatroban (0.1-1 μM) for 4 h.

  • (Only for Reference)
Animal Research:

[2]

  • Animal Models: Mice that were injected with MDA-231 breast cancer cells into the left heart ventricle
  • Dosages: 9 mg/kg/day
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(189.87 mM)
Ethanol 40 mg/mL
(75.95 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 526.65
Formula

C23H36N6O5S.H2O

CAS No. 141396-28-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CCN(C(C1)C(=O)O)C(=O)C(CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C.O

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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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