1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPF-04995274Cat. No.: HY-18137CAS No.: 1331782-27-4分式: CHNO分量: 432.51作靶點: 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (231.2

2、1 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3121 mL 11.5604 mL 23.1209 mL5 mM 0.4624 mL 2.3121 mL 4.6242 mL10 mM 0.2312 mL 1.1560 mL 2.3121 mL請根據(jù)產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 PF-04995274種強效，親和，服活性素 4 受體 (5-HT4R) 的部分激動劑。PF-04995274 對 5-

3、HT4A/4B/4D/4E 的 EC50 范為 0.26-0.47 nM (Ki 范為 0.15-0.46 nM)，對 5-HT4S/4L/4E 的 EC50 范圍為 0.59-0.65 nM ( 5-HT4S 的 Ki 為 0.30 nM)。PF-04995274腦滲透的，可于治療與阿爾茨海默癥相關的認知障礙。IC50 & Target 5-HT4 receptor 1 2 31/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 PF-04995274 has EC50 values of 0.47 nM, 0.36 nM, 0.37 n

4、M, 0.26 nM, 0.59 nM, 0.65 nM and 0.62 nM forhuman 5-HT4A/4B/4D/4E and rat 5-HT4S/4L/4E, respectively. PF-04995274 has Ki values of 0.36 nM, 0.46nM, 0.15 nM, 0.32 nM and 0.3nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S, respectively 3.體內研究 PF-04995274 (3-10 mg/kg; intravenous injection; for 17 days; ma

5、le 129S6/SvEv mice) treatment results inprophylactic efficacy by attenuating learned fear and decreasing stress-induced depressive-like behavior 1.Animal Model: Male 129S6/SvEv mice (7-8 weeks) treated with contextual fear conditioning (CFC) andforced swim test (FST) 1Dosage: 3 mg/kg, 10 mg/kgAdmini

6、stration: Intravenous injection; for 17 daysResult: Attenuated learned fear and decreased stress-induced depressive-like behavior.REFERENCES1. Chen BK, et al. Prophylactic efficacy of 5-HT4R agonists against stress. Neuropsychopharmacology. 2019 Oct 10.2. Grimwood S, et al. Translational receptor oc

7、cupancy for the 5-HT4 partial agonist PF-04995274 in rats, non-human primates andhealthy volunteers. Alzheimers Dement: J Alzheimers Assoc. 2011;7:S653.3. Timothy Nicholas1, et al. Systems pharmacology modeling in neuroscience: Prediction and outcome of PF-04995274, a 5-HT4 partialagonist, in a clinical scopolamine impairment trial. Advances in Alzheimers Disease. Vol.2 No.3(2013).McePdfHeightCaution: Product has not been fully validated for medical applications.For resear