PF-04995274 是强效,高亲和力,口服活性血清素 4 受体的部分激动剂。它是可脑渗透的,可用于与阿尔茨海默症相关的认知障碍的研究。
产品描述
PF-04995274 is an effective, high-affinity, and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM). It also has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S).
体外活性
PF-04995274 shows Ki values of 0.36 nM, 0.46 nM, 0.15 nM, 0.32 nM and 0.3nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S, respectively. PF-04995274 displays EC50 values of 0.47 nM, 0.36 nM, 0.37 nM, 0.26 nM, 0.59 nM, 0.65 nM and 0.62 nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S/4L/4E, respectively [3].
体内活性
PF-04995274 (3-10 mg/kg; intravenous injection; for 17 days; male 129S6/SvEv mice) treatment causes prophylactic efficacy by attenuating learned fear. It also decreasing stress-induced depressive-like behavior[1].
Cas No.
1331782-27-4
分子式
C23H32N2O6
分子量
432.51
别名
PF-04995274
储存和溶解度
DMSO:100 mg/mL (231.21 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years