(Rac)-Tavapadon((Rac)-PF-06649751;(Rac)-CVL-751)是有效的，选择性非儿茶酚多巴胺D1受体(dopamineD1receptor)激动剂。(Rac)-Tavapadon在GS激活试验中显示出强大的完全激动作用，在β-arrestin2募集试验中显示出部分激动作用(GS-cAMP,EC50=0.8nM;β-arrestin2,EC50=68nM)。(Rac)-Tavapadon具有抗帕金森病活性。
货号:ajcx29022
CAS:1643462-64-9
分子式:C19H16F3N3O3
分子量：391.34
溶解度:DMSO: 41.67 mg/mL (106.48 mM); H2O:< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity[1].

(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751; compound 32) has EMAXs of 118% and 30% in the GS activation assay and the β-arrestin2 recruitment assay[1].

[1]. Michael L Martini, et al. Designing Functionally Selective Noncatechol Dopamine D 1 Receptor Agonists with Potent In Vivo Antiparkinsonian Activity. ACS Chem Neurosci. 2019 Sep 18;10(9):4160-4182.