Purity ~92% (HPLC). A cell-permeable quinolinimine compound that acts as a selective, potent blocker of G-protein coupled receptors (GPCR) that contain a constrained eighth helix (H8). The inhibition is selective and blocks G-protein signaling mediated via Gaq, but not Ga12. A non-orthosteric antagonist of PAR1 (IC50=4uM) that is shown to inhibit PAR1 and CCR-4 induced platelet aggregation without affecting PAR4 mediated aggregation. Shown to inhibit thrombus formation following vascular injury (IC50 ~1mg/kg). Also acts as a potent, non-competitive blocker of a2A-adrenergic receptors (IC50=2.5uM as shown by a decrease in 3H-yohimbine binding). Formula: C17H22N2 · HI Solubility: DMSO Molecular Weight: 382.3