| 中文名称 |
Perzinfotel
|
| 英文名称 |
Perzinfotel
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| 英文别名 |
Phosphonic acid,P-[2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)ethyl]-;P-[2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)ethyl]-phosphonic acid;EAA-090;Perzinfotel;WAY-126090;FX5AUU7Z8T;(2-(8,9-Dioxo-2,6-diazabicyclo(5.2.0)non-1(7)-en-2-yl)ethyl)phosphonic acid;EAA 090;Way 126090;Perzinfotel (USAN/INN);Perzinfotel [USAN:INN];per-zinfotel;[2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)ethyl]phosphonic acid;BDBM86494;DB12365;D05447;Q7171293
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| Cas No. |
144912-63-0
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| 分子式 |
C9H13N2O5P
|
| 分子量 |
260.18
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
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| 详情描述 |
Perzinfotel (EAA-090) 是一种有效选择性的,竞争性的 NMDA 受体拮抗剂,具有神经保护作用。Perzinfotel (EAA-090) 对谷氨酸位点显示出高亲和力 (IC50=30 nM)。
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| 产品详情 |
Perzinfotel (EAA-090) 是一种有效选择性的,竞争性的 NMDA 受体拮抗剂,具有神经保护作用。Perzinfotel (EAA-090) 对谷氨酸位点显示出高亲和力 (IC50=30 nM)。
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| 生物活性 |
Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC 50 =30 nM) for the glutamate site.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
NMDA receptor
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| 体外研究(In Vitro) |
Perzinfotel blocks NMDA-induced currents with an IC50 of 0.48 μM and glutamate-induced neurotoxicity with an IC50 of 1.6 μM. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
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| ClinicalTrial |
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| 参考文献 |
[1]. Brandt MR, et al. Effects of the N-methyl-D-aspartate receptor antagonist perzinfotel [EAA-090; [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid] on chemically induced thermal hypersensitivity. J Pharmacol Exp Ther. 2005 Jun;31[2]. Kinney WA, et al. Design and synthesis of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid(EAA-090), a potent N-methyl-D-aspartate antagonist, via the use of 3-cyclobutene-1,2-dione as an achiral alpha-amino acid bioisostere. J
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| 溶解度数据 |
In Vitro: DMSO : 20.83 mg/mL (80.06 mM; Need ultrasonic)H2O : 5.88 mg/mL (22.60 mM; ultrasonic and warming and heat to 60°C)配制储备液
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[1]. Brandt MR, et al. Effects of the N-methyl-D-aspartate receptor antagonist perzinfotel [EAA-090; [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid] on chemically induced thermal hypersensitivity. J Pharmacol Exp Ther. 2005 Jun;31[2]. Kinney WA, et al. Design and synthesis of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid(EAA-090), a potent N-methyl-D-aspartate antagonist, via the use of 3-cyclobutene-1,2-dione as an achiral alpha-amino acid bioisostere. J
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。