| Name | AZD1283 |
| Description | AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM). AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses induced the increase in bleeding time at 33 and 100 μg/kg/min for 3- and 13-fold, respectively. Thus, the therapeutic index (TI) was ≥10 for both compounds. |
| In vivo | Acute administration of dasotraline dose-dependently decreases the spontaneous firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of α2, D2 and 5-HT1A autoreceptors, respectively. Dasotraline predominantly inhibits the firing rate of LC NE neurons while producing only a partial decrease in VTA DA and DR 5-HT neuronal discharge. SEP-225289 is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE[1]. Average dopamine and serotonin transporter occupancies increase with increasing doses of SEP-225289. Mean dopamine and serotonin transporter occupancies are 33%±11% and 2%±13%, respectively, for 8 mg; 44%±4% and 9%±10%, respectively, for 12 mg; and 49%±7% and 14%±15%, respectively, for 16 mg[2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.25 mM), Sonication is recommended.
DMSO : 22.5 mg/mL (47.82 mM), Sonication is recommended.
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| Keywords | thromboembolic | P2YReceptor | P2Y12 | P2Y Receptor | P2Y | Inhibitor | inhibit | AZD-1283 | AZD1283 | AZD 1283 | antithrombotic | antiplatelet aggregation |
| Inhibitors Related | Prasugrel Hydrochloride | Prasugrel | Sodium metatungstate | Regrelor disodium | (±) Clopidogrel hydrogen sulfate | Uridine-5'-diphosphate disodium salt | Uridine triphosphate trisodium salt | ATPγS tetralithium salt | P2Y1/P2Y12 antagonist-1 | Ticagrelor | Diquafosol tetrasodium | cangrelor tetrasodium |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Obesity Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Preclinical Compound Library | GPCR Compound Library | Anti-Cancer Compound Library |
United States
