A phenoxypyridinyl-phenylurea that acts as a highly selective P2Y1 antagonist (Ki = 6nM against 0.5nM 2-MeS-ADP for human P2Y1 binding), while displaying much reduced or no affinity toward other P2Y family GPCRs (Ki = ≥2.5uM toward hP2Y14; Ki >15uM toward human P2Y2, P2Y6, P2Y11, and P2Y12). Effectively inhibits 2.5uM ADP-induced platelet aggregation in vitro (IC50 = 2.1uM) and reduces FeCl2-induced carotid artery blood clot formation in anesthetized rats in vivo (10mg/kg/h i.v. infusion) with much less effect toward prolonging cuticle and mesenteric bleeding time when compared to another P2Y12 antagonist Clopidogrel. Pharmackinetic studies reveal only moderate oral bioavailability in rat.
Molecular Formula:C₂₃H₂₂F₃N₃O₃
Solubility:DMSO
Primary Target:P2Y1
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
