PF-06256142 是一种高效、选择性的，中枢神经系统穿透性的，具有口服活性的 D1 受体 (D1 receptor) 激动剂，其 EC50 和 Ki 值分别为 33 nM 和 12 nM。PF-06256142 有用于精神分裂症和阿尔茨海默症研究的潜力。
货号:ajcx39396
CAS:1609583-14-3
分子式:C21H16N4O2S
分子量：388.44
溶解度:DMSO : 200 mg/mL (514.88 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease[1].

PF-06256142 exhibits IC50 values of 10 μM)[1].

PF-06256142 exhibits high oral bioavailability (rat 85%) following oral administration (rat 5 mg/kg)[1].PF-06256142 exhibits terminal elimination half-life (rat 2.3 h) following intravenous administration (rat 5.0 mg/kg)[1].

[1]. Davoren JE, et al. Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. J Med Chem. 2018 Nov 15.

Protocol:

HumanD1Receptor 33nM(EC50)