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| Targets |
MRS1523 targets the adenosine A₃ receptor (A₃AR), a G protein-coupled receptor (GPCR) that is activated by adenosine. A₃ receptors are involved in various physiological processes, including inflammation, cardioprotection, and neurotransmission. MRS1523 acts as a potent and selective antagonist at the A₃AR, with Kᵢ values of 18.9 nM for the human receptor and 113 nM for the rat receptor. It demonstrates strong selectivity over A₁ and A₂A receptors. By blocking A₃AR, MRS1523 can be used to study the role of this receptor in various disease models.
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| 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].
In vitro, MRS1523 potently inhibits A₃ receptor-mediated signaling in cell-based assays. In A₃AR-expressing cells, the compound inhibits agonist-stimulated cAMP accumulation, calcium mobilization, or GTPγS binding. The compound's selectivity for A₃AR over A₁ and A₂A receptors has been confirmed in receptor binding and functional assays. MRS1523 is a valuable tool for studying A₃ receptor function and the role of adenosine signaling in various physiological and pathological processes. |
| 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].
In vivo, MRS1523 has been used in neuronal studies to investigate the role of A₃ receptors in the central nervous system. As a selective A₃AR antagonist, it can block the effects of A₃ receptor agonists in animal models. The compound has been used to study the involvement of A₃ receptors in pain, inflammation, neuroprotection, and other conditions. Specific in vivo efficacy data are available from published studies. MRS1523 is a research tool and has not been developed for clinical applications. |
| Enzyme Assay |
In vitro receptor binding assays for MRS1523 typically involve competition binding studies using radiolabeled A₃ receptor ligands. A typical protocol: membrane preparations from cells expressing human or rat A₃AR are incubated with [¹²⁵I]-ABA (an A₃ receptor agonist) and varying concentrations of MRS1523 (0.01 nM to 10 μM) in binding buffer for 60-90 minutes at room temperature. Non-specific binding is determined in the presence of 10 μM unlabeled agonist. Bound radioactivity is separated by rapid filtration and quantified by scintillation counting. Kᵢ values are calculated from competition curves using nonlinear regression. Each concentration is tested in triplicate.
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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. In vitro cell-based assays for MRS1523 are performed using A₃AR-expressing cell lines such as CHO-A₃AR or HEK293-A₃AR. A typical protocol: cells are seeded in 96-well plates and cultured overnight. Cells are pre-incubated with MRS1523 at concentrations ranging from 0.01 nM to 10 μM for 30 minutes. Cells are then stimulated with an A₃ receptor agonist (e.g., Cl-IB-MECA) for 15-30 minutes. Signaling readouts include cAMP accumulation (measured by ELISA or HTRF), calcium mobilization (measured using Fluo-4 or Fura-2 AM), or GTPγS binding. Antagonistic activity is expressed as the percent inhibition of agonist-stimulated signaling. |
| Animal Protocol |
In vivo animal studies for MRS1523 are conducted in rodent models of pain, inflammation, or neurological disorders. A typical protocol: male Sprague-Dawley rats or C57BL/6 mice are administered MRS1523 via intraperitoneal or intracerebroventricular injection at doses of 0.1-10 mg/kg. For pain studies, analgesic effects are assessed using the formalin test or hot plate test. For inflammation studies, inflammatory markers are measured. The compound is typically administered 15-30 minutes before testing. Efficacy is assessed by comparing responses between treatment and vehicle control groups.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MRS1523 have not been fully characterized. The compound is soluble in DMSO. Its plasma half-life, volume of distribution, protein binding, and oral bioavailability remain unknown. The compound is a research-grade chemical and has not been developed for clinical applications. It is primarily used for in vitro and in vivo studies of adenosine receptor pharmacology. The compound should be stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Toxicological data for MRS1523 are limited. As a research chemical, it has not undergone formal toxicology testing. Standard laboratory safety precautions should be followed when handling MRS1523: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The compound should be stored at -20°C for long-term stability. No genotoxicity, carcinogenicity, or reproductive toxicity data are available. Researchers should consult the safety data sheet (SDS) before handling.
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| References |
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| Additional Infomation |
Additional information for MRS1523: The compound has a CAS number of 212329-37-8. Its molecular formula is C₂₃H₂₉NO₃S and molecular weight is 399.55 g/mol. It is a potent and selective adenosine A₃ receptor antagonist. Kᵢ values: 18.9 nM (human) and 113 nM (rat). It is selective over A₁ and A₂A receptors. It is for research use only and is not approved for clinical applications. No FDA approvals exist.
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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
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| 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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