P2Y Antagonist II (1-(2-(2-tert-Butylphenoxy)pyridin-3-yl)-3-(4-(trifluoromethoxy)phenyl)urea, Purinergic Receptor P2Y Antagonist II)

Size

£522.00

SKU:: 217615
Purity:: ≥99% (HPLC)
Storage Conditions:: 4°C
Supplier:: United States Biological
Format:: Supplied as a white powder.
Extra Details:: 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.