化合物AZD1283 T3536

Product Introduction
Bioactivity


英文名: AZD1283

描述: AZD1283是P2Y12受体拮抗剂，EC50为3.0 ug/kg/min，结合的IC50为11 nM。它剂量依赖性地诱导血流量增加和抑制 ADP 诱导的血小板聚集，抗血栓形成的 ED50 值分别为 3.0 和 10 μg/kg/min。

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 22.5 mg/mL (47.82 mM)


关键字: P2Y Receptor | thromboembolic | antiplatelet aggregation | AZD1283 | inhibit | Inhibitor | antithrombotic | AZD 1283 | AZD-1283

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相关库: Anti-COVID-19 Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Inhibitor Library | Anti-Obesity Compound Library | Target-Focused Phenotypic Screening Library | Preclinical Compound Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library

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