MRS 1220

• Catalog No.: M228
• CAS Number: 183721-15-5
• M. F.: C21H14ClN5O2
• M. W.: 403.82116

SYNONYMS

• IUPAC name: N-[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide
• IUPAC Traditional name: N-[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide
• Synonyms: 9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline

DATABASE IDS

• MDL Number: MFCD01321046
• PubChem SID: 24896720
• CAS Number: 183721-15-5

PROPERTIES

• Gene Information: human ... ADORA3(140)rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
• Apperance: white solid
• Solubility: DMSO: soluble2 mg/mL
• Solubility: 2-hydroxypropyl-β-cyclodextrin: insoluble
• Solubility: H2O: insoluble
• Solubility: ethanol: insoluble
• Personal Protective Equipment: Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter
• German water hazard class: 3

DETAILS

Description (English)

Biochem/physiol Actions
MRS1220 is a putative A3 adenosine receptor antagonist. MRS 1220 was found to be competitive in saturation binding studies using the agonist radioligand 125I AB-MECA at cloned human brain A3 receptors expressed in HEK-293 cells. Antagonism was demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of 35S guanosine 5′-O-(3-thiotriphosphate (35S GTP-gamma-S) to the associated G-proteins. MRS 1220 and MRS 1191, with KB values of 1.7 and 92 nM, respectively, proved to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase. In addition, MRS 1220 reversed the effect of A3 agonist-elicited inhibition of tumor necrosis factor-alpha formation in the human macrophage U-937 cell line, with an IC50 value of 0.3 μM.