HA2A/hCA XII modulator 1

HA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research[1].

Product Specifications

CAS Number

[2548963-55-7]

UNSPSC

12352005

Target

Adenosine Receptor; Carbonic Anhydrase

Type

Reference compound

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ha2a-hca-xii-modulator-1.html

Solubility

10 mM in DMSO

Smiles

O=C(NC1=CC=C(C2=CN3C(C(N)=N2)=NN(C4=CC=CC=C4)C3=O)C=C1)C5=CC=C(S(=O)(N)=O)C=C5

Molecular Formula

C24H19N7O4S

Molecular Weight

501.52

References & Citations

[1]Costanza Ceni, et al. Discovery of first-in-class multi-target adenosine A 2A receptor antagonists-carbonic anhydrase IX and XII inhibitors. 8-Amino-6-aryl-2-phenyl-1,2,4-triazolo [4,3-a]pyrazin-3-one derivatives as new potential antitumor agents. Eur J Med Chem. 2020 Sep 1;201:112478.