化合物PF-04995274 T16481

Product Introduction
Bioactivity


英文名: PF-04995274

描述: 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。

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].

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

溶解度: DMSO : 100 mg/mL (231.21 mM)


关键字: Inhibitor | 5-HT4 | 5-hydroxytryptamine Receptor | behavior | Alzheimer′s disease | PF04995274 | inhibit | PF 04995274 | Serotonin Receptor | 5-HT Receptor | PF-04995274 | Stress-induced | depressive-like

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相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Neurotransmitter Receptor Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | CNS-Penetrant Compound Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | NO PAINS Compound Library

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