Argatroban

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Description: Potent thrombin inhibitor
Chemical Name: (2R,4R)-1-[(2S)-5-[(aminoiminomethyl)amino]-1-oxo-2-[[(1,2,3,4-tetrahydro-3-methyl-8-quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2-piperidinecarboxylic acid
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews

Biological Activity for Argatroban

Argatroban is a potent inhibitor of thrombin mediated fibrinogen cleavage (Ki = 19 nM). Competitive inhibitor of thrombin-induced platelet activation and clotting. Shown to exhibit antithrombotic activity in animal models.

This compound is a mixture of 2 diastereomers (approximate ratio 65/35).

Compound Libraries for Argatroban

Argatroban is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Argatroban

M. Wt 508.63
Formula C23H36N6O5S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 74863-84-6
PubChem ID 6604954
InChI Key CQTDZUSQSTUZDA-UHFFFAOYSA-M
Smiles O=C(N1[C@@H]([C@@](O)=O)C[C@H](C)CC1)[C@@H](NS(C2=CC=CC3=C2NCC(C)C3)(=O)=O)CCCNC(N)=N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Argatroban

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.86 100
1eq. HCl 5.09 10

Preparing Stock Solutions for Argatroban

The following data is based on the product molecular weight 508.63. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.97 mL 9.83 mL 19.66 mL
5 mM 0.39 mL 1.97 mL 3.93 mL
10 mM 0.2 mL 0.98 mL 1.97 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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References for Argatroban

References are publications that support the biological activity of the product.

Kikumoto et al (1984) Selective inhibition of thrombin by (2R,4R)-4-methyl-1-[N2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl++ +) sulfonyl]-1-arginyl)]-2-piperidinecarboxylic acid. Biochemistry 23 85 PMID: 6691968

Jang et al (1990) Prevention of platelet-rich arterial thrombosis by selective thrombin inhibition. Circulation 81 219 PMID: 2297828

Fitzgerald and Fitzgerald (1989) Role of thrombin and thromboxane A2 in reocclusion following coronary thrombolysis with tissue-type plasminogen activator. Proc.Natl.Acad.Sci.USA 86 7585


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Keywords: Argatroban, Argatroban supplier, Potent, inhibitors, thrombin, fibrinogen, inhibits, antithrombitic, Other, Proteases, 1637, Tocris Bioscience

Citations for Argatroban

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