(S)-CPW 399
目录号 : GC17313
AMPA agonist,subtype-selective,weakly desensitizing
Cas No.:389888-02-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(S)-CPW 399 is a potent and selective agonist of AMPA receptor with Ki value of 747 nM [1].
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA receptor) is an ionotropic transmembrane receptor for glutamate and mediates fast synaptic transmission in the central nervous system. AMPA receptors are oligomeric assemblies of four protein subunits, GluR1-4.
(S)-CPW 399 is a potent and selective AMPA receptor agonist. (S)-CPW 399 exhibited affinity with Ki values of 109, 218, 2137 and 1756 nM for GluR1, GluR2, GluR3 and GluR4 receptors, respectively [1]. In mouse cerebellar granule cells, (S)-CPW 399 induced neuronal cell death in a concentration- and time-dependent way with EC50 value of 70 μM and increased intracellular free-calcium levels ([Ca2+]i ) in a concentration-dependent way with EC50 value of 5 μM [2]. In rat cerebellar granule cells, CPW-399 increased the expression of GABAA receptor δ subunit, which relied on NMDA receptor activation [3]. In Sf9 cells expressing iGluR5, (S)-CPW 399 exhibited affinity for iGluR5 with Ki value of 44 nM. In Xenopus læVis Oocytes, (S)-CPW 399 exhibited agonist activity with EC50 values of 24.9, 13.9, 224 and 34.3 μM for iGluR1, iGluR2, iGluR3 and iGluR4 receptors, respectively [4].
References:
[1]. Campiani G, Morelli E, Nacci V, et al. Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399 as a novel, potent, and subtype-selective AMPA receptor full agonist with partial desensitization properties. J Med Chem, 2001, 44(26): 4501-4504.
[2]. Sinclair C, Reavy H, Grieve A, et al. Inherent desensitisation-preventing properties of a novel, subtype-selective AMPA receptor agonist, (S)-CPW 399, as a possible explanation for its excitotoxic action in cultured cerebellar granule cells. Neurochem Int, 2003, 42(6): 499-510.
[3]. Salonen V, Kallinen S, Lopez-Picon FR, et al. AMPA/kainate receptor-mediated up-regulation of GABAA receptor delta subunit mRNA expression in cultured rat cerebellar granule cells is dependent on NMDA receptor activation. Brain Res, 2006, 1087(1): 33-40.
[4]. Butini S, Pickering DS, Morelli E, et al. 1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators. J Med Chem, 2008, 51(20): 6614-6618.
| Cas No. | 389888-02-2 | SDF | |
| 化学名 | (S)-2-amino-3-(2,4-dioxo-2,3,4,5,6,7-hexahydro-1H-cyclopenta[d]pyrimidin-1-yl)propanoic acid | ||
| Canonical SMILES | O=C1NC(N(C[C@@H](C(O)=O)N)C2=C1CCC2)=O | ||
| 分子式 | C10H13N3O4 | 分子量 | 239.23 |
| 溶解度 | <11.96mg/ml in Water | 储存条件 | Desiccate at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1801 mL | 20.9004 mL | 41.8008 mL |
| 5 mM | 0.836 mL | 4.1801 mL | 8.3602 mL |
| 10 mM | 0.418 mL | 2.09 mL | 4.1801 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。