Home Proteases Thrombin inhibitor Argatroban Monohydrate For research use only.

Argatroban Monohydrate

Synonyms: Argatroban hydrate, Argipidine,MCI-9038 Monohydrate

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

Argatroban Monohydrate Chemical Structure

Argatroban Monohydrate Chemical Structure

CAS: 141396-28-3

Selleck's Argatroban Monohydrate has been cited by 2 publications

Purity & Quality Control

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

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Biological Activity

Description Argatroban (Argatroban hydrate, Argipidine,MCI-9038 Monohydrate) is a direct, selective thrombin inhibitor with anticoagulant effects.
Targets
thrombin [1]
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research 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.

Chemical lnformation & Solubility

Molecular Weight 526.65 Formula

C23H36N6O5S.H2O
CAS No. 141396-28-3 SDF --
Smiles CC1CCN(C(C1)C(=O)O)C(=O)C(CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C.O
Storage (From the date of receipt)

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


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In vivo
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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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