| Size | Price | Stock | Qty |
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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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| 1g |
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Purity: ≥98%
Argatroban hydrate (also known as 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 individuals 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.
| ln Vitro |
Because of its single target specificity for thrombin, argatroban (MD-805) may have a complementing effect in avoiding thrombosis without aggravating bleeding tendencies. In order to treat traumatic aortic rupture associated with multi-organ injury during left heart bypass surgery, a safe anticoagulant called argatroban (MD-805) is injected at a rate of 0.5 to 2 mcg/kg/minute [1]. Argatroban (MD-805) appears to improve TPA reperfusion in patients with AMI, especially those who present later than expected, as compared to heparin. Argatroban-treated patients experience fewer serious bleeding episodes and worse clinical outcomes [2].
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| ln Vivo |
Argatroban monohydrate can be utilized in animal modeling to produce endogenous intestinal embolism models.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Because argatroban is poorly absorbed orally, it might not adversely affect a breastfeeding infant. However, no information is available on the use of argatroban during breastfeeding, so an alternate drug is preferred. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
Argatroban is an Anti-coagulant and Direct Thrombin Inhibitor. The mechanism of action of argatroban is as a Thrombin Inhibitor.
Argatroban is a synthetic derivative of L-arginine with antithrombotic activity. Argatroban is a univalent and direct inhibitor of fibrin-bound thrombin. This agent reversibly binds to the thrombin active site thereby preventing the thrombin-dependent reactions, which include conversion of fibrinogen to fibrin; the activation of factors V, VIII and XI; the activation of protein C; and platelet aggregation. Argatroban is highly selective for thrombin and is able to inhibit the action of both free and clot-associated thrombin. As a result, stabilization of blood clots and coagulation is inhibited. |
| Molecular Formula |
C23H38N6O6S
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|---|---|
| Molecular Weight |
526.653
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| Exact Mass |
508.24679
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| Elemental Analysis |
C, 52.45; H, 7.27; N, 15.96; O, 18.23; S, 6.09
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| CAS # |
141396-28-3
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| Related CAS # |
Argatroban;74863-84-6
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| PubChem CID |
92721
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
801.3±75.0 °C at 760 mmHg
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| Melting Point |
-41.5 °C
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| Flash Point |
438.4±37.1 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.674
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| LogP |
2.56
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
36
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| Complexity |
887
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| Defined Atom Stereocenter Count |
3
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| SMILES |
S(C1=C([H])C([H])=C([H])C2=C1N([H])C([H])([H])C([H])(C([H])([H])[H])C2([H])[H])(N([H])[C@@]([H])(C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H])C(N1C([H])([H])C([H])([H])[C@@]([H])(C([H])([H])[H])C([H])([H])[C@]1([H])C(=O)O[H])=O)(=O)=O.O([H])[H]
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| InChi Key |
AIEZTKLTLCMZIA-CZSXTPSTSA-N
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| 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
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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;hydrate
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| Synonyms |
MCI-9038; MCI9038; MCI9038; MD-805; MD 805; MD805; DK-7419; DK7419; DK 7419; GN1600; GN-1600; GN 1600; MMTQAP; MPQA; Novastan; Argatroban; OM 805; Argipidine; Slonnon
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ≥ 100 mg/mL (~189.88 mM)
H2O : ~1 mg/mL (~1.90 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8988 mL | 9.4940 mL | 18.9879 mL | |
| 5 mM | 0.3798 mL | 1.8988 mL | 3.7976 mL | |
| 10 mM | 0.1899 mL | 0.9494 mL | 1.8988 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.
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