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MRS1523 is a novel, potent and selective antagonist of A3 adenosine receptor with Ki of 18.9 nM and 113 nM for human and rat A3 receptors, respectively
| ln Vitro |
Thirty minutes prior to the administration of cordycepin (60 μM), treatment with MRS 1523 (0.1-1 μM) dramatically reduced the number of cells, 40.7% and 57.4% of control values, respectively. MRS1523 (1 μM) acts alone to influence the development of tumor cells [3]. MRS 1523 (1 nM) treatment of human endothelial progenitor cells (hEPC) resulted in a partial suppression of adenosine 5'-N-ethylformamide (NECA)-induced migration. Additionally, in 3-day-old hEPCs, treatment with MRS 1523 at a concentration of 100 nM reduced NECA-induced migration by 70%. MRS 1523 inhibits NECA-induced migration in a dose-response fashion, with an estimated Ki of 147 nM [4].
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| ln Vivo |
The excitability of small to medium-sized, capsaicin-sensitive dorsal root ganglion (DRG) neurons isolated from 3- to 4-week-old rats was investigated, together with the expression and functional consequences of the A3 adenosine receptor (A3AR). N-type Ca currents are decreased by the endogenous agonist adenosine; however, the presence of the A3AR antagonist MRS 1523 inhibits this action by 56%. A3AR activation in MRS also dramatically decreased rat DRG neuronal activity in a way that was 1523-sensitive but PD173212-insensitive, according to current-clamp recordings [2].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: B16-BL6 Cell Tested Concentrations: 0.1 µM, 1 µM Incubation Duration: 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: Antagonizes growth inhibition caused by cordycepin. |
| References |
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| Molecular Formula |
C23H29NO3S
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|---|---|
| Molecular Weight |
399.54626
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| Exact Mass |
399.187
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| CAS # |
212329-37-8
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| PubChem CID |
3661570
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| Appearance |
Colorless to light yellow ointment
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| Density |
1.1g/cm3
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| Boiling Point |
551.3ºC at 760 mmHg
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| Flash Point |
287.2ºC
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| Index of Refraction |
1.554
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| LogP |
5.723
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
28
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| Complexity |
492
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCC1=C(C(=NC(=C1C(=O)OCCC)C2=CC=CC=C2)CC)C(=O)SCC
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| InChi Key |
UUSHFEVEROROSP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H29NO3S/c1-5-12-17-19(23(26)28-8-4)18(7-3)24-21(16-13-10-9-11-14-16)20(17)22(25)27-15-6-2/h9-11,13-14H,5-8,12,15H2,1-4H3
|
| Chemical Name |
propyl 6-ethyl-5-ethylsulfanylcarbonyl-2-phenyl-4-propylpyridine-3-carboxylate
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| Synonyms |
MRS1523 MRS 1523 MRS-1523.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~250.28 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5028 mL | 12.5141 mL | 25.0282 mL | |
| 5 mM | 0.5006 mL | 2.5028 mL | 5.0056 mL | |
| 10 mM | 0.2503 mL | 1.2514 mL | 2.5028 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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