Melagatran
Based on 1 Customer Validation
Melagatran is a reversible, selective, orally active direct inhibitor of thrombin with a Ki of 2 nM. Melagatran binds directly to the active site of thrombin, inhibiting thrombin-mediated conversion of fibrinogen to fibrin. Melagatran reduces the DNA binding activity of NF-κB and AP-1. Melagatran reduces fibrin deposition in organs, alleviates ischemic brain damage, and reduces the size of advanced atherosclerotic lesions. Melagatran can be used in the study of cardiovascular disease (coronary thrombosis, atherosclerosis) and ischemic brain damage.
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- Pureté: 99.31%
- CAS No.: 159776-70-2
- Formule: C22H31N5O4
- Masse moléculaire:429.51
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Ki: 2 nM (Thrombin)[1]
Melagatran (1.5-2.5 mg/kg; p.o. via nasogastric tube) prevents or delays electrically induced occlusive thrombus formation in the canine left anterior descending coronary artery[2].
Melagatran (10 μmol/kg; p.o.) shows good oral bioavailability (61%-74%) in dogs[3].
Melagatran (loading dose of 0.3 μmol/kg followed by infusion of 0.1-5 μmol/kg/h for 30 min; administered immediately, 1-6 h after middle cerebral artery (MCA) occlusion) reduces ischemic brain injury in rats in a dose-dependent and time-dependent manner[5].
Melagatran (500 μmol/kg diet; p.o. via chow diet; 22 weeks for apolipoprotein E–deficient mice, 8 weeks for C57BL/6J mice) reduces advanced atherosclerotic lesion size and promotes plaque stability in apolipoprotein E–deficient mice, but has no significant effect on early lesion formation in C57BL/6J mice[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female anaesthetised endotoxaemic pigs (endotoxaemic model induced by infusion of Escherichia coli endotoxin 0111: B4 at 8 µg/kg/h for 6 h)[1]
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Dosage:0.3 mg/kg iv bolus followed by 0.1 mg/kg/h iv infusion
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Administration:Intravenous bolus injection followed by continuous intravenous infusion; 3 h infusion period
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Result:Counteracted the progressive increase in pulmonary capillary wedge pressure (PCWP) and decrease in left ventricular stroke work index (LVSWI) induced by endotoxin.
Significantly alleviated the endotoxin-induced decrease in systemic vascular resistance index (SVRI) by 30% at 2 h.
Maintained plasma creatinine and increases urine output.
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Animal Model:Apolipoprotein E-deficient mice (strain name B6.129P2 on a C57BL/6J background), 30-week-old females[6].
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Dosage:500 μmol/kg/d melagatran mixed in chow diet
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Administration:Oral administration via chow diet; 22 weeks
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Result:Significantly reduced maximum lesion area (234876 μm² vs. 290733 μm² in control group), maximum stenosis (71.5% vs. 78.0% in control group), and maximum lesion thickness (274 μm vs. 365 μm in control group).
Increased fibrous cap thickness (28.4 μm vs. 20.8 μm in control group) and media thickness (29.3 μm vs. 24.4 μm in control group).
Reduced necrotic core size (73537 μm² vs. 126819 μm² in control group).
Decreased DNA binding activity of NF-κB and AP-1.
Chemical Information
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CAS No. 159776-70-2
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Appearance Solid
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Masse moléculaire 429.51
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Formule C22H31N5O4
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Color White to off-white
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SMILES
NC(C(C=C1)=CC=C1CNC([C@@H]2CCN2C([C@@H](C3CCCCC3)NCC(O)=O)=O)=O)=N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 175 mg/mL (407.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Eriksson M, et al. Effects of melagatran, a novel direct thrombin inhibitor, during experimental septic shock. Expert Opin Investig Drugs. 2000 May;9(5):1129-37. [Content Brief]
[2]. Mehta JL, et al. Melagatran, an oral active-site inhibitor of thrombin, prevents or delays formation of electrically induced occlusive thrombus in the canine coronary artery. J Cardiovasc Pharmacol. 1998 Mar;31(3):345-51. [Content Brief]
[3]. Gustafsson D, et al. Effects of melagatran, a new low-molecular-weight thrombin inhibitor, on thrombin and fibrinolytic enzymes. Thromb Haemost. 1998 Jan;79(1):110-8. [Content Brief]
[4]. Elg M, et al. Antithrombotic effects and bleeding time of thrombin inhibitors and warfarin in the rat. Thromb Res. 1999 May 1;94(3):187-97. [Content Brief]
[5]. Wang CX, et al. Treatment with melagatran alone or in combination with thrombolytic therapy reduced ischemic brain injury. Exp Neurol. 2008 Sep;213(1):171-5. [Content Brief]
[6]. Bea F, et al. Melagatran reduces advanced atherosclerotic lesion size and may promote plaque stability in apolipoprotein E-deficient mice. Arterioscler Thromb Vasc Biol. 2006 Dec;26(12):2787-92. [Content Brief]
[7]. Ainscow EK, et al. Investigations into the liver effects of ximelagatran using high content screening of primary human hepatocyte cultures. Expert Opin Drug Saf. 2008 Jul;7(4):351-65. [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. 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 | 2.3282 mL | 11.6412 mL | 23.2823 mL | 58.2059 mL |
| 5 mM | 0.4656 mL | 2.3282 mL | 4.6565 mL | 11.6412 mL | |
| 10 mM | 0.2328 mL | 1.1641 mL | 2.3282 mL | 5.8206 mL | |
| 15 mM | 0.1552 mL | 0.7761 mL | 1.5522 mL | 3.8804 mL | |
| 20 mM | 0.1164 mL | 0.5821 mL | 1.1641 mL | 2.9103 mL | |
| 25 mM | 0.0931 mL | 0.4656 mL | 0.9313 mL | 2.3282 mL | |
| 30 mM | 0.0776 mL | 0.3880 mL | 0.7761 mL | 1.9402 mL | |
| 40 mM | 0.0582 mL | 0.2910 mL | 0.5821 mL | 1.4551 mL | |
| 50 mM | 0.0466 mL | 0.2328 mL | 0.4656 mL | 1.1641 mL | |
| 60 mM | 0.0388 mL | 0.1940 mL | 0.3880 mL | 0.9701 mL | |
| 80 mM | 0.0291 mL | 0.1455 mL | 0.2910 mL | 0.7276 mL | |
| 100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.5821 mL |
Melagatran Related Classifications
HY-129056 Related Classifications
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