| Bioactivity | P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes[1]. | ||||||||||||
| Target | IC50: 1.67 µM (GPR17), 3.17 µM (P2Y2R) | ||||||||||||
| Name | P2Y2R/GPR17 antagonist 1 | ||||||||||||
| CAS | 2395016-49-4 | ||||||||||||
| Formula | C19H13ClN2O6S | ||||||||||||
| Molar Mass | 432.83 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Pillaiyar T, et al. Design, synthesis and biological evaluation of suramin-derived dual antagonists of the proinflammatory G protein-coupled receptors P2Y2 and GPR17. Eur J Med Chem. 2020 Jan 15;186:111789. |