Pesampator (PF-04958242) 是一种有效的、高选择性的AMPA受体的正变构调节剂 (AMPA 增强剂),EC50为 310 nM,Ki为 170 nM。
生物活性 | Pesampator (PF-04958242) is a potent and highly selective positive allosteric modulator ofAMPA receptor(an AMPA potentiator) with anEC50of 310 nM and aKiof 170 nM[1]. |
体内研究 (In Vivo) | Pesampator (0.1-1 mg/kg; SC) dose-dependently increases CD-1 mouse cerebellum cGMP and Pesampator (0.1-0.32 mg/kg; SC) decreases fall latency in C57BL/6J mice traversing an accelerating rotarod[1]. Pesampator (0.001-0.01 mg/kg; male Sprague-Dawley rats) reverses the MK-801-mediated (0.05 mg/kg; IV) reduction in paired-pulse facilitation (PPF) after cumulative or a single (0.01 mg/kg) intravenous dose[1]. Pesampator (0.0032–0.032 mg/kg; SC) attenuates ketamine-induced working memory disruptions in rats as determined by mean errors in a radial arm maze[1]. In rats, Pesampator (0.027, 0.08, and 0.60 mg/kg; SC) dose-dependently affectes the regional brain uptake of 2-deoxy-2-[18F]fluoro-d-glucose (FDG)[1].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(254.78 mM;Need ultrasonic) 配制储备液 1 mM | 2.5478 mL | 12.7392 mL | 25.4784 mL | 5 mM | 0.5096 mL | 2.5478 mL | 5.0957 mL | 10 mM | 0.2548 mL | 1.2739 mL | 2.5478 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |