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MRS 1220_Molecular_structure_CAS_183721-15-5)
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MRS 1220

Catalog No. M228 Name Sigma Aldrich
CAS Number 183721-15-5 Website http://www.sigmaaldrich.com
M. F. C21H14ClN5O2 Telephone 1-800-521-8956
M. W. 403.82116 Fax
Purity Email
Storage Chembase ID: 132285


IUPAC name
IUPAC Traditional name


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


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


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.