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MRS-1706

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Catalog No. T16136Cas No. 264622-53-9

MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B receptor inverse agonist.

MRS-1706

MRS-1706

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Purity: 99.00%
Catalog No. T16136Cas No. 264622-53-9
MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B receptor inverse agonist.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$31In StockIn Stock
5 mg$72In StockIn Stock
10 mg$122In StockIn Stock
25 mg$247In StockIn Stock
50 mg$396In StockIn Stock
100 mg$635-In Stock
200 mg$893-In Stock
1 mL x 10 mM (in DMSO)$80In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.00%
Appearance:Solid
Color:White
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Product Introduction

MRS-1706 AI Summary
MRS-1706 exhibits a range of bioactivities related to both adenosine receptors and cytochrome P450 enzymes. It acts as an antagonist on various adenosine receptor subtypes, including A1, A2A, A2B, and A3, with Ki values of 157.0 nM, 112.0 nM, 1.39 nM, and 230.0 nM, respectively. The highest affinity is observed for the A2B adenosine receptor. Selectivity ratios indicate a notable preference for the A3 receptor over the A2B receptor, with a ratio of 170.0, suggesting significant potential pharmacological effects mediated through adenosine receptor modulation. In addition, MRS-1706 shows inhibitory effects on cytochrome P450 enzymes, specifically 2C19, 2D6, and 2C9. It demonstrates potent inhibition of Cytochrome P450 2D6 with an IC50 of 100.0 nM, and less potent inhibition of Cytochrome P450 2C9 with an IC50 of 39810.7 nM. In panel assays, it has AC50 values of 7943.28 nM for 2C19 and 39810.72 nM for 2C9, confirming its activity against these enzymes. These properties suggest that MRS-1706 could have various therapeutic applications through adenosine receptor antagonism and cytochrome P450 enzyme inhibition..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B receptor inverse agonist.
Targets&IC50
A2 receptor (human):157(ki), A2A receptor (human):112(ki), A2B receptor (human):(ki)1.39 , A3 receptor (human):230 nM
Chemical Properties
Molecular Weight503.55
FormulaC27H29N5O5
Cas No.264622-53-9
SmilesCCCn1c2[nH]c(nc2c(=O)n(CCC)c1=O)-c1ccc(OCC(=O)Nc2ccc(cc2)C(C)=O)cc1
Relative Density.1.293 g/cm3 (Predicted)
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 6.4 mg/mL (12.71 mM), Sonication and heating are recommended.
H2O: < 0.1 mg/mL (insoluble)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.99 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9859 mL9.9295 mL19.8590 mL99.2950 mL
5 mM0.3972 mL1.9859 mL3.9718 mL19.8590 mL
10 mM0.1986 mL0.9930 mL1.9859 mL9.9295 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Dose Conversion

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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

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