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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 297 | 现货 | |
5 mg | ¥ 663 | 现货 | |
10 mg | ¥ 1,090 | 现货 | |
25 mg | ¥ 1,960 | 现货 | |
50 mg | ¥ 3,190 | 现货 | |
100 mg | ¥ 4,580 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 629 | 现货 |
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]. |
分子量 | 432.51 |
分子式 | C23H32N2O6 |
CAS No. | 1331782-27-4 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (231.21 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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