Argatroban hydrate
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MedKoo CAT#: 319512

CAS#: 141396-28-3 (hydrate)

Description: Argatroban is an anticoagulant that is a direct thrombin inhibitor. Argatroban was approved in 2000 for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT). Argatroban is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; activation of protein C; and platelet aggregation. Argatroban inhibits thrombin with an inhibition constant (Ki) of 0.04 μM.


Chemical Structure

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Argatroban hydrate
CAS# 141396-28-3 (hydrate)

Theoretical Analysis

MedKoo Cat#: 319512
Name: Argatroban hydrate
CAS#: 141396-28-3 (hydrate)
Chemical Formula: C23H38N6O6S
Exact Mass: 508.24679
Molecular Weight: 526.653
Elemental Analysis: C, 52.45; H, 7.27; N, 15.96; O, 18.23; S, 6.09

Price and Availability

Size Price Availability Quantity
100.0mg USD 350.0 2 Weeks
200.0mg USD 550.0 2 Weeks
500.0mg USD 1250.0 2 Weeks
1.0g USD 2250.0 2 Weeks
2.0g USD 4050.0 2 Weeks
5.0g USD 6950.0 2 Weeks
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Related CAS #: 74863-84-6 (anhydrous)   141396-28-3 (hydrate)    

Synonym: MCI-9038; MCI9038; MCI9038; MD805; MD-805; MD 805; DK-7419; DK 7419; DK7419; GN1600; GN-1600; GN 1600; MMTQAP; MPQA; Argatroban.Novastan; OM 805; Slonnon; Argipidine.

IUPAC/Chemical Name: (2R,4R)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(3R)-3-methyl-1,2,3,4-tetrahydroquinolin-8-yl]sulfonylamino]pentanoyl]-4-methyl-piperidine-2-carboxylic acid hydrate

InChi Key: AIEZTKLTLCMZIA-VJCHTHLQSA-N

InChi Code: InChI=1S/C23H36N6O5S.H2O/c1-14-8-10-29(18(12-14)22(31)32)21(30)17(6-4-9-26-23(24)25)28-35(33,34)19-7-3-5-16-11-15(2)13-27-20(16)19;/h3,5,7,14-15,17-18,27-28H,4,6,8-13H2,1-2H3,(H,31,32)(H4,24,25,26);1H2/t14-,15-,17+,18-;/m1./s1

SMILES Code: O=C([C@@H]1N(C([C@@H](NS(=O)(C2=CC=CC3=C2NC[C@H](C)C3)=O)CCC/N=C(N)\N)=O)CC[C@@H](C)C1)O.[H]O[H]

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 526.653 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Grouzi E. Update on argatroban for the prophylaxis and treatment of heparin-induced thrombocytopenia type II. J Blood Med. 2014 Aug 13;5:131-41. doi: 10.2147/JBM.S38762. eCollection 2014. Review. PubMed PMID: 25152637; PubMed Central PMCID: PMC4140228.

2: Rozec B, Boissier E, Godier A, Cinotti R, Stephan F, Blanloeil Y. [Argatroban, a new antithrombotic treatment for heparin-induced thrombocytopenia application in cardiac surgery and in intensive care]. Ann Fr Anesth Reanim. 2014 Sep-Oct;33(9-10):514-23. doi: 10.1016/j.annfar.2014.06.006. Epub 2014 Aug 20. Review. French. PubMed PMID: 25148720.

3: Badiye A, Hernandez GA, Chaparro S. Argatroban as novel therapy for suspected thrombosis in patients with continuous-flow left ventricle assist device and hemolysis. ASAIO J. 2014 May-Jun;60(3):361-5. doi: 10.1097/MAT.0000000000000067. Review. PubMed PMID: 24614354.

4: Argatroban: for a few selected patients. Prescrire Int. 2013 Feb;22(135):33-5. Review. PubMed PMID: 23444494.

5: Cruz-González I, López-Jiménez R, Perez-Rivera A, Yan BP. Pharmacokinetic evaluation of argatroban for the treatment of acute coronary syndrome. Expert Opin Drug Metab Toxicol. 2012 Nov;8(11):1483-93. doi: 10.1517/17425255.2012.722621. Epub 2012 Sep 13. Review. PubMed PMID: 22970706.

6: Alatri A, Armstrong AE, Greinacher A, Koster A, Kozek-Langenecker SA, Lancé MD, Link A, Nielsen JD, Sandset PM, Spanjersberg AJ, Spannagl M. Results of a consensus meeting on the use of argatroban in patients with heparin-induced thrombocytopenia requiring antithrombotic therapy - a European Perspective. Thromb Res. 2012 Apr;129(4):426-33. doi: 10.1016/j.thromres.2011.11.041. Epub 2011 Dec 16. Review. PubMed PMID: 22178575.

7: Jeske WP, Fareed J, Hoppensteadt DA, Lewis B, Walenga JM. Pharmacology of argatroban. Expert Rev Hematol. 2010 Oct;3(5):527-39. doi: 10.1586/ehm.10.53. Review. PubMed PMID: 21083469.

8: Babuin L, Pengo V. Argatroban in the management of heparin-induced thrombocytopenia. Vasc Health Risk Manag. 2010 Sep 7;6:813-9. Review. PubMed PMID: 20859550; PubMed Central PMCID: PMC2941792.

9: Follis F, Filippone G, Montalbano G, Floriano M, Lobianco E, D'Ancona G, Follis M. Argatroban as a substitute of heparin during cardiopulmonary bypass: a safe alternative? Interact Cardiovasc Thorac Surg. 2010 Apr;10(4):592-6. doi: 10.1510/icvts.2009.215848. Epub 2010 Jan 8. Review. PubMed PMID: 20061338.

10: Dhillon S. Argatroban: a review of its use in the management of heparin-induced thrombocytopenia. Am J Cardiovasc Drugs. 2009;9(4):261-82. doi: 10.2165/1120090-000000000-00000. Review. PubMed PMID: 19655821.

11: Hursting MJ, Soffer J. Reducing harm associated with anticoagulation: practical considerations of argatroban therapy in heparin-induced thrombocytopenia. Drug Saf. 2009;32(3):203-18. doi: 10.2165/00002018-200932030-00003. Review. PubMed PMID: 19338378.

12: Taimeh Z, Weksler B. Review: recent advances in argatroban-warfarin transition in patients with heparin-induced thrombocytopenia. Clin Appl Thromb Hemost. 2010 Feb;16(1):5-12. doi: 10.1177/1076029608327862. Epub 2008 Dec 2. Review. PubMed PMID: 19054792.

13: Young SK, Al-Mondhiry HA, Vaida SJ, Ambrose A, Botti JJ. Successful use of argatroban during the third trimester of pregnancy: case report and review of the literature. Pharmacotherapy. 2008 Dec;28(12):1531-6. doi: 10.1592/phco.28.12.1531. Review. PubMed PMID: 19025434.

14: Boggio LN, Oza VM. Argatroban use in heparin-induced thrombocytopenia. Expert Opin Pharmacother. 2008 Aug;9(11):1963-7. doi: 10.1517/14656566.9.11.1963 . Review. PubMed PMID: 18627333.

15: Ohtani R, Tomimoto H, Takahashi R, Tsukahara T, Hatano T. [Argatroban]. Nihon Rinsho. 2006 Oct 28;64 Suppl 7:581-4. Review. Japanese. PubMed PMID: 17461209.

16: Martin ME, Kloecker GH, Laber DA. Argatroban for anticoagulation during cardiac surgery. Eur J Haematol. 2007 Feb;78(2):161-6. Review. PubMed PMID: 17328717.

17: Schönfeld H, Hein OV. [Pharmacotherapy: argatroban--alternative to heparin in case of heparin-induced thrombocytopenia type II (HIT II)]. Anasthesiol Intensivmed Notfallmed Schmerzther. 2006 Jun;41(6):376-7. Review. German. PubMed PMID: 16804787.

18: Yeh RW, Jang IK. Argatroban: update. Am Heart J. 2006 Jun;151(6):1131-8. Review. PubMed PMID: 16781211.

19: Escolar G, Bozzo J, Maragall S. Argatroban: a direct thrombin inhibitor with reliable and predictable anticoagulant actions. Drugs Today (Barc). 2006 Apr;42(4):223-36. Review. PubMed PMID: 16703119.

20: Matthai WH Jr. Safety and efficacy of argatroban in patients with heparin-induced thrombocytopenia. Curr Hematol Rep. 2006 Mar;5(1):95-9. Review. PubMed PMID: 16537053.