Argatroban monohydrate
Based on 5 publication(s) in Google Scholar
Argatroban (monohydrate) (MD-805 (monohydrate)) is a direct, selective thrombin inhibitor.
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- Pureza: 99.57%
- No. CAS: 141396-28-3
- Fòrmula: C23H38N6O6S
- Peso molecular:526.65
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Argatroban monohydrate
More
Actividad biológica
Thrombin[1].
Argatroban (MD-805) may have a complementary effect for preventing thrombus formation without aggravating bleeding tendency because of its monotarget specificity to thrombin. Administration (0.5 to 2 micrograms/kg/min) of Argatroban (MD-805) is a safe anticoagulant for left heart bypass in repairs of traumatic aortic rupture associated with multiple organ injuries[1]. Argatroban (MD-805), as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation. The incidences of major bleeding and adverse clinical outcome were lower in the patients receiving argatroban[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.
Argatroban monohydrate is suitable for creating animal models to thrombolysis. In rats that have undergone hepatectomy, the pharmacokinetic parameters of Argatroban, such as area under the curve, volume of distribution, and elimination half-life, are significantly increased. Argatroban is converted from the 21-(R) isomer to the 21-(S) enantiomer in the kidneys, the latter exhibiting greater antithrombotic activity and potentially being more readily cleared by the liver[4].
Administration: 30 mg/kg • SC • daily for 16 weeks.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 141396-28-3
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Appearance Solid
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Peso molecular 526.65
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Fòrmula C23H38N6O6S
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Color White to off-white
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SMILES
O=C([C@@H]1N(C([C@@H](NS(=O)(C2=CC=CC3=C2NCC(C)C3)=O)CCCNC(N)=N)=O)CC[C@@H](C)C1)O.O
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Synonyms
MD-805 monohydrate; MCI-9038 monohydrate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (5)
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Journal Impact Factor
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Most Recent
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Int Immunopharmacol
Argatroban and Menadione exert protective effects in ultraviolet-irradiated skin inflammation: A transcriptomic analysis based on identification of iron overload related biomarkers. [Abstract]2025 Apr 4:151:114334. PMID: 40020462 -
Int J Mol Sci
A Combined Activity of Thrombin and P-Selectin Is Essential for Platelet Activation by Pancreatic Cancer Cells. [Abstract]2021 Mar 24;22(7):3323. PMID: 33805059 -
Antiviral Res
Omicsynin B4 potently blocks coronavirus infection by inhibiting host proteases cathepsin L and TMPRSS2. [Abstract]2023 Jun:214:105606. PMID: 37076089 -
Biomed Pharmacother
Drug repositioning: Identification of potent inhibitors of NS3 protease and NS5 RdRp for control of DENV infection. [Abstract]2025 Apr 28:187:118104. PMID: 40300391 -
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (189.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kawada, T., et al., Argatroban, an attractive anticoagulant, for left heart bypass with centrifugal pump for repair of traumatic aortic rupture. Jpn J Thorac Cardiovasc Surg, 1999. 47(3): p. 104-9. [Content Brief]
[2]. Jang, I.K., et al., A multicenter, randomized study of argatroban versus heparin as adjunct to tissue plasminogen activator (TPA) in acute myocardial infarction: myocardial infarction with novastan and TPA (MINT) study. J Am Coll Cardiol, 1999. 33(7): p. 1879-85. [Content Brief]
[3]. Hashimoto M, et al. Suppression of argatroban-induced endogenous thrombolysis by PKSI-527, and antibodies to TPA and UPA, evaluated in a rat arterial thrombolysis model. Thromb Haemost. 2003 May;89(5):820-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8988 mL | 9.4940 mL | 18.9879 mL | 47.4699 mL |
| 5 mM | 0.3798 mL | 1.8988 mL | 3.7976 mL | 9.4940 mL | |
| 10 mM | 0.1899 mL | 0.9494 mL | 1.8988 mL | 4.7470 mL | |
| 15 mM | 0.1266 mL | 0.6329 mL | 1.2659 mL | 3.1647 mL | |
| 20 mM | 0.0949 mL | 0.4747 mL | 0.9494 mL | 2.3735 mL | |
| 25 mM | 0.0760 mL | 0.3798 mL | 0.7595 mL | 1.8988 mL | |
| 30 mM | 0.0633 mL | 0.3165 mL | 0.6329 mL | 1.5823 mL | |
| 40 mM | 0.0475 mL | 0.2373 mL | 0.4747 mL | 1.1867 mL | |
| 50 mM | 0.0380 mL | 0.1899 mL | 0.3798 mL | 0.9494 mL | |
| 60 mM | 0.0316 mL | 0.1582 mL | 0.3165 mL | 0.7912 mL | |
| 80 mM | 0.0237 mL | 0.1187 mL | 0.2373 mL | 0.5934 mL | |
| 100 mM | 0.0190 mL | 0.0949 mL | 0.1899 mL | 0.4747 mL |
Argatroban monohydrate Related Classifications
HY-B0375A Related Classifications
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