2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Thrombin NF-κB AP-1
  4. Melagatran

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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Melagatran

Melagatran Chemical Structure

CAS No. : 159776-70-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Melagatran Related Antibodies

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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c-Fos FosB Fra1/FOSL1 Fra2/FOSL2 c-Jun

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Description

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[1][2][3][4][5][6][7].

IC50 & Target

Ki: 2 nM (Thrombin)[1]
In Vitro

Melagatran shows a low inhibition constant (Ki = 2 nM) for thrombin[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Melagatran Related Antibodies
In Vivo

Melagatran (0.3 mg/kg iv bolus followed by 0.1 mg/kg/h iv infusion for 3 h) alleviates endotoxin-induced systemic haemodynamic disorders, protects renal function, and reduces intra-organ fibrin deposition in anaesthetised endotoxaemic pigs[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.

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]
Dosage: 0.3 mg/kg iv bolus followed by 0.1 mg/kg/h iv infusion
Administration: Intravenous bolus injection followed by continuous intravenous infusion; 3 h infusion period
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.
Animal Model: Apolipoprotein E-deficient mice (strain name B6.129P2 on a C57BL/6J background), 30-week-old females[6].
Dosage: 500 μmol/kg/d melagatran mixed in chow diet
Administration: Oral administration via chow diet; 22 weeks
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.
Molecular Weight

429.51

Formula

C22H31N5O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC(C(C=C1)=CC=C1CNC([C@@H]2CCN2C([C@@H](C3CCCCC3)NCC(O)=O)=O)=O)=N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3282 mL 11.6412 mL 23.2823 mL
5 mM 0.4656 mL 2.3282 mL 4.6565 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.31%

SDS (251 KB)

COA (246 KB) HNMR (268 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

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
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Melagatran Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Melagatran159776-70-2ThrombinNF-κBAP-1Nuclear factor-κBNuclear factor-kappaBActivator Protein 1Inhibitorinhibitorinhibit

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