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Melagatran

Name: Melagatran
Brand: TargetMol
SKU: T11994
Price: 540 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11994Cas No. 159776-70-2

Melagatran is an orally available, direct synthetic thrombin inhibitor that does not require endogenous cofactors other than thrombin and does not significantly interact with any other enzymes in the coagulation cascade or with the fibrinolytic enzymes.

Melagatran

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Purity: 99.83%

Catalog No. T11994Cas No. 159776-70-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$540	In Stock	In Stock
5 mg	$1,260	In Stock	In Stock
10 mg	$1,630	In Stock	In Stock
25 mg	$2,460	In Stock	In Stock
50 mg	$3,290	In Stock	In Stock
100 mg	$4,470	-	In Stock
1 mL x 10 mM (in DMSO)	$1,190	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.83%

ee:100%

Appearance:Solid

Color:White

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COA LCMS CSFC HNMR

Product Introduction

Melagatran AI Summary

Melagatran exhibits potent inhibitory activity against human thrombin with a Ki value of 2.0 nM and an IC50 value ranging from 4.7 to 4700 nM, depending on the assay conditions. It has a high binding affinity for thrombin, suggesting significant inhibitory effects on thrombin activity. In addition to thrombin, Melagatran demonstrates inhibition of other coagulation factors such as plasmin (IC50 = 3060.0 nM), trypsin (IC50 = 11.9 nM), factor IXa, and factor Xa (IC50 = 17300.0 nM), and exhibits antithrombin activity in both rats and dogs, with respective oral bioavailability F values of 5.2% and 24.0%. Pharmacokinetic studies indicate moderate volume of distribution, high fraction unbound in plasma, and moderate clearance rates in humans. It also demonstrates low oral bioavailability (3.0%) and low permeability across human Caco2 cells (Papp = 0.03 ucm/s). Additionally, Melagatran shows antiviral activity against SARS-CoV-2 but with a high IC50 (>20000 nM). Despite moderate inhibition of other targets like plasmin and tissue-type plasminogen activator, it remains a promising candidate for therapeutic applications related to anticoagulation..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

In vivo

METHODS: To test the hypothesis that a regimen consisting of an oral thrombin inhibitor would delay or prevent occlusive clot formation, anesthetized dogs were given melagatran (1.5, 2.5 mg/kg) via nasogastric tube, and 15 minutes later, a potent thrombogenic stimulus in the form of an anodic current (100 μA) was applied to the intimal surface of the stenotic left anterior descending coronary artery (LAD).
RESULTS One of the dogs given high-dose melagatran did not develop thrombotic occlusion of the LAD during the entire 4-hour observation period. In the melagatran-treated dogs, coronary artery occlusions occurred during the observation period in 68% (low-dose) and 75% (high-dose) of the dogs.[2]

Chemical Properties

Molecular Weight	429.51
Formula	C₂₂H₃₁N₅O₄
Cas No.	159776-70-2
Smiles	C([C@H](NCC(O)=O)C1CCCCC1)(=O)N2[C@H](C(NCC3=CC=C(C(=N)N)C=C3)=O)CC2
Relative Density.	1.41 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (104.77 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3282 mL	11.6412 mL	23.2823 mL	116.4117 mL
5 mM	0.4656 mL	2.3282 mL	4.6565 mL	23.2823 mL
10 mM	0.2328 mL	1.1641 mL	2.3282 mL	11.6412 mL
20 mM	0.1164 mL	0.5821 mL	1.1641 mL	5.8206 mL
50 mM	0.0466 mL	0.2328 mL	0.4656 mL	2.3282 mL
100 mM	0.0233 mL	0.1164 mL	0.2328 mL	1.1641 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc