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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Argatroban (MD-805; MCI-9038; Argipidine) is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM. Argatroban is a thrombin inhibitor that is used as an anticoagulant. In 2000, the FDA approved argatroban for the prevention or treatment of thrombosis in patients suffering from heparin-induced thrombocytopenia (HIT). Argatroban binds to the thrombin active site reversibly and functions as a direct thrombin inhibitor. Argatroban inhibits thrombin-catalyzed or -induced reactions, such as fibrin formation, the activation of coagulation factors V, VIII, and XIII, the activation of protein C, and platelet aggregation, to produce its anticoagulant effects.
Targets |
Thrombin (Ki = 5-39 nM)
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ln Vitro |
Argatroban is a potent and selective synthetic thrombin inhibitor with Ki values against thrombin ranging from 5 nM to 39 nM. In numerous animal models of thrombosis that is both platelet-rich and erythrocyte-rich, argatroban exhibits antithrombotic characteristics. Argatroban inhibits thrombus formation in a dose-dependent manner; in this test, its estimated ED50 was 125 μg/kg. Argatroban increases thrombin time in a dose-dependent manner; at the highest dose used, this increase was 511%, but the APTT increased only by 73%.[1] Argatroban has the ability to directly cause vascular smooth muscle cells to change phenotype, which leads to an increase in the mRNAs for SMemb, PAI-1, and beta-actin.[2]
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ln Vivo |
Argatroban prevents the growth of microthrombi for three hours following middle cerebral artery (MCA) occlusion; after that, it has no further effect. Six hours following MCA occlusion, argatroban also significantly reduces the size of ischemic cerebral lesions. In [3] In the rat model of distal middle cerebral artery occlusion, argatroban (0.3 mg/h/rat) significantly reduces the number of microthrombi 1 day after distal middle cerebral artery (dMCA) occlusion. One day after distal middle cerebral artery (dMCA) occlusion, a reduction in regional cerebral blood flow (rCBF) is significantly reversed by argatroban (0.1 and 0.3 mg/h/rat). Argatroban (0.3 mg/h/rat) also greatly diminishes the cerebral infarction's size.[4]
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Animal Protocol |
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References |
Molecular Formula |
C23H36N6O5S
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Molecular Weight |
508.63
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Exact Mass |
508.2468
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Elemental Analysis |
C, 54.31; H, 7.13; N, 16.52; O, 15.73; S, 6.30
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CAS # |
74863-84-6
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Appearance |
Solid powder
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SMILES |
C[C@@H]1CCN([C@H](C1)C(=O)O)C(=O)[C@H](CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C
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InChi Key |
KXNPVXPOPUZYGB-IOVMHBDKSA-N
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InChi Code |
InChI=1S/C23H36N6O5S/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)/t14-,15?,17+,18-/m1/s1
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Chemical Name |
(2R,4R)-1-[(2S)-5-(diaminomethylideneamino)-2-[(3-methyl-1,2,3,4-tetrahydroquinolin-8-yl)sulfonylamino]pentanoyl]-4-methylpiperidine-2-carboxylic acid
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
2% DMSO+40% PEG 300+2% Tween 80+ddH2O: 5mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9661 mL | 9.8303 mL | 19.6607 mL | |
5 mM | 0.3932 mL | 1.9661 mL | 3.9321 mL | |
10 mM | 0.1966 mL | 0.9830 mL | 1.9661 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05226442 | Recruiting | Drug: Unfractionated heparin Drug: Argatroban |
Extracorporeal Membrane Oxygenation Complication Anticoagulants and Bleeding Disorders |
Medical University of Vienna | December 1, 2021 | Phase 2 Phase 3 |
NCT04925167 | Recruiting | Drug: unfractionated heparin Drug: Argatroban |
Respiratory Failure | Beijing Chao Yang Hospital | July 6, 2021 | Not Applicable |
NCT03735979 | Active Recruiting |
Drug: Argatroban Drug: Eptifibatide |
Acute Ischemic Stroke | Washington University School of Medicine |
October 15, 2019 | Phase 3 |
NCT00039858 | Completed | Drug: Argatroban | Thrombocytopenia Thrombosis |
Encysive Pharmaceuticals | September 2003 | Phase 4 |
NCT05325346 | Completed | Drug: VLX-1005 Drug: Argatroban |
Heparin-induced Thrombocytopenia | Veralox Therapeutics | March 7, 2022 | Phase 1 |