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MRS1220

CAS No. 183721-15-5

MRS1220( —— )

Catalog No. M33892 CAS No. 183721-15-5

MRS1220, a selective and potent antagonist for the human A3 adenosine receptor (hA3AR) with a dissociation constant (Ki) of 0.59 nM, exhibits therapeutic promise for central nervous system disease research.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    MRS1220
  • Note
    Research use only, not for human use.
  • Brief Description
    MRS1220, a selective and potent antagonist for the human A3 adenosine receptor (hA3AR) with a dissociation constant (Ki) of 0.59 nM, exhibits therapeutic promise for central nervous system disease research.
  • Description
    MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo.
  • In Vitro
    MRS 1220 reverses the effect of A3 agonist-elicited inhibition of tumor necrosis factor-α formation in the human macrophage U-937 cell line with an IC50 of 0.3 μM.VEGF secretion in U87MG glioblastoma stem-like cells (GSCs) decreases ~25% with MRS1220 after 72 h of hypoxia.Cell Viability Assay Cell Line:U87MG GSCs Concentration:10 μM Incubation Time:72 hours Result:Decreased ~25% VEGF secretion.
  • In Vivo
    MRS1220 (0.15 mg/kg; intraperitoneal inoculation) reduces tumor size and blood vessel formation in vivo. MRS1220 exhibits a strong in vivo anti-angiogenic effect.Animal Model:Eight, 8 week-old male Sprague-Dawley rats bearing C6 (GSCs) Dosage:0.15 mg/kg/72 h Administration:Administered by intraperitoneal inoculation, for fifteen days Result:A reduction close to 80% and 90% in tumor volume compared to the vehicle-treated group at day ten and fifteen post-treatment, respectively.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    Adenosine Receptor
  • Recptor
    Adenosine Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    183721-15-5
  • Formula Weight
    403.82
  • Molecular Formula
    C21H14ClN5O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 4 mg/mL (9.91 mM; Ultrasonic (<60°C)
  • SMILES
    Clc1ccc2nc(NC(=O)Cc3ccccc3)n3nc(nc3c2c1)-c1ccco1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. K A Jacobson, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.?
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