PEAQX (NVP-AAM077) tetrasodium hydrate 是有效的、选择性的、口服有效的NMDA拮抗剂,其对hNMDAR 1A/2A和hNMDAR 1A/2B的IC50值分别为 270 nM 和 29600 nM。
生物活性 | PEAQX (NVP-AAM077) tetrasodium hydrate is a potent, selective and orally activeNMDAantagonist, withIC50values of 270 nM and 29600 nM forhNMDAR 1A/2BandhNMDAR 1A/2B, respectively[1]. |
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体外研究 (In Vitro) | PEAQX (3 μM) produces similar caspase-3 activation, while NVP-AAM007 is approximately three-fold more potent[2].
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体内研究 (In Vivo) | PEAQX (10-40 mg/kg) dose-dependently increased cortical caspase-3 activity following sub-chronic administration[2]. PEAQX (10 and 20 mg/kg) shows enhanced locomotor activity in response to PCP challenge (4 mg/kg on PN28-35) compared to saline pretreatment (F3, 73=4.99)[2]. PEAQX (10 mg/kg, ip) antagonizes the effects of PRE084 on CaMKIV-TORC1-CREB and BDNF, even for learning and memory impairment[3].
Animal Model: | Timed, day 14 pregnant female Sprague-Dawley rats[2]. | Dosage: | 10, 20 or 40 mg/kg. | Administration: | S.C. | Result: | Showed a sensitized locomotor response to PCP challenge on PN28-35. |
Animal Model: | Timed, day 14 pregnant female Sprague-Dawley rats[2]. | Dosage: | 4 mg/kg. | Administration: | I.P. | Result: | Did not significantly increase locomotor activity in rats treated sub-chronically with PEAQX on PN7, 9 and 11. |
Animal Model: | 11-week old C57BL/6 mice[3]. | Dosage: | 10 mg/kg. | Administration: | IP. | Result: | Reversed the effect of PRE084 (F3,78= 10.446, p<0.01). |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : 25.5 mg/mL(45.52 mM;Need ultrasonic and warming) 配制储备液 1 mM | 1.7852 mL | 8.9262 mL | 17.8524 mL | 5 mM | 0.3570 mL | 1.7852 mL | 3.5705 mL | 10 mM | 0.1785 mL | 0.8926 mL | 1.7852 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 (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 100 mg/mL (178.52 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |