1. GPCR/G Protein
  2. Adenosine Receptor
  3. MRS-1191

MRS-1191 

Cat. No.: HY-124543
Handling Instructions

MRS-1191 is a potent and selective A3 adenosine receptor antagonist with a KB value of 92 nM, a Ki value of 31.4 nM for human A3 receptor and an IC50 of 120 nM for CHO cells.

For research use only. We do not sell to patients.

MRS-1191 Chemical Structure

MRS-1191 Chemical Structure

CAS No. : 185222-90-6

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Description

MRS-1191 is a potent and selective A3 adenosine receptor antagonist with a KB value of 92 nM, a Ki value of 31.4 nM for human A3 receptor and an IC50 of 120 nM for CHO cells[1].

IC50 & Target

Ki: 31.4 nM (human A3 adenosine receptor)[1]

In Vitro

The effects of putative A3 adenosine receptor antagonist of MRS-1191 is characterized in receptor binding and functional assays. MRS-1191 is found to be competitive in saturation binding studies using the agonist radioligand [125I]AB-MECA (N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide) at cloned human brain A3 receptor expressed in HEK-293 cells. Antagonism is 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-1191 with a KB value of 92 nM, proves to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase[1].

Molecular Weight

477.55

Formula

C₃₁H₂₇NO₄

CAS No.

185222-90-6

SMILES

O=C(OCC)C1=C(NC(C2=CC=CC=C2)=C(C1C#CC3=CC=CC=C3)C(OCC4=CC=CC=C4)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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MRS-1191
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