Name: MRS1523
Price: 198.00 USD

- Overview
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    Background
    
    Ki = 18.9 nM for human adenosine A3 receptorKi = 113 nM for rat adenosine A3 receptorMRS1523 is a selective adenosine A3 receptor (A3R) antagonist. A3R is strongly overexpressed in cancer cell lines and cancer tissues. The activation of the A3R is related to several second messenger systems which are for signaling pathways including asthmatic, inflammatory, and ischemic responses.In vitro: MRS1523 reversed the increase in mRNA expression in B16-F10 Melanoma Cells. Also, MRS1523 antagonized the modulation in the expression level of the proteins, which indicated that adenosine A3R mediated the responses [1].In vivo: C57BL/6J, male mice, inoculated B16-F10 melanoma cells, were administered MRS1523 at a dose of 100 μg/kg orally twice daily for 15 days. MRS1523 counteracted the activity of IB-MECA which is an adenosine A3R agonist. In addition, it was demonstrated that the response was adenosine A3R mediated. The modulation of up-regulation of GSK-3β expression level was neutralized by MRS1523, further suggesting the specificity of the response [1].
- Properties
  - Categories
    
    adenosine A3 receptor antagonist
    
    Alternative Name
    
    6-ethyl-5-[(ethylthio)carbonyl]-2-phenyl-4-propyl-3-pyridinecarboxylic acid propyl ester
    
    CAS Number
    
    212329-37-8
    
    Molecular Formula
    
    C23H29NO3S
    
    Molecular Weight
    
    399.5
    
    Appearance
    
    A solution in ethanol. To change the solvent, simply evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤50mg/ml in DMSO;50mg/ml in dimethyl formamide
    
    Storage
    
    Supplied as a solution in ethanol,Store at -20°C
    
    SMILES
    
    CCCOC(C1=C(CCC)C(C(SCC)=O)=C(CC)N=C1C2=CC=CC=C2)=O
    
    * For Research Use Only
- Reference
  - 1. Hui Bai, Zhiheng Zhang, et al. "Activation of adenosine A3 receptor attenuates progression of osteoarthritis through inhibiting the NLRP3/caspase-1/GSDMD induced signalling." J Cell Mol Med. 2022 Aug;26(15):4230-4243. PMID: 35775127