| CAS NO: | 157604-55-2 |
| 包装: | 5mg |
| 市场价: | 2760元 |
| Physical Appearance | White solid |
| Storage | Desiccate at RT |
| M.Wt | 505.61 |
| Cas No. | 157604-55-2 |
| Formula | C30H35NO6 |
| Solubility | <25.28mg/ml in ethanol;<50.56mg/ml in DMSO |
| Chemical Name | (S)-1-(2-(tris(4-methoxyphenyl)methoxy)ethyl)piperidine-3-carboxylic acid |
| Canonical SMILES | OC([C@@H]1CN(CCOC(C(C=C2)=CC=C2OC)(C(C=C3)=CC=C3OC)C(C=C4)=CC=C4OC)CCC1)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
(S)-SNAP 5114是一种选择性的GABA转运体抑制剂,对hGAT-3\rGAT-2及hGAT-1的IC50值分别为5\21及388 μM[1].
γ-氨基丁酸(GABA)在中枢神经系统(CNS)中是主要的抑制性神经递质,对亨廷顿病\帕金森病\癫痫\精神分裂症及阿尔兹海默症起到至关重要的作用.GABA转运蛋白将GABA从胶质细胞和神经细胞外侧转运到细胞内侧[2].
(S)-SNAP 5114是一种选择性的GABA转运体抑制剂.在表达mGAT1-4的HEK-293细胞系中,(S)-SNAP 5114对mGAT1\mGAT3及mGAT4 具有抑制能力,pIC50值分别为4.07\5.29及5.71,且抑制56%的mGAT2[2].在丘脑中,SNAP-5114 (100 μM)将GABA水平增加至247%.在经最大电休克的幼鼠中,SNAP-5114抑制后肢强直性伸展.在DBA/2小鼠中,SNAP-5114剂量依赖性地抑制声诱发惊厥,ED50值为110 μmol/kg [3].在大鼠中,SNAP5114 (10\50\100或200 μg)抑制福尔马林试验中的迟发相反应,延长甩尾实验中的撤退潜伏期,这表明,SNAP5114抑制化学和热伤害感受.在慢性缩窄性损伤大鼠中,SNAP5114剂量依赖性地抑制机械性痛觉过敏[4].
参考文献：
[1]. Borden LA, Dhar TG, Smith KE, et al. Cloning of the human homologue of the GABA transporter GAT-3 and identification of a novel inhibitor with selectivity for this site. Receptors Channels, 1994, 2(3): 207-213.
[2]. Pabel J, Faust M, Prehn C, et al. Development of an (S)-1-{2-[tris(4-methoxyphenyl)methoxy]ethyl}piperidine-3-carboxylic acid [(S)-SNAP-5114] carba analogue inhibitor for murine γ-aminobutyric acid transporter type 4. ChemMedChem, 2012, 7(7): 1245-1255.
[3]. Dalby NO. GABA-level increasing and anticonvulsant effects of three different GABA uptake inhibitors. Neuropharmacology, 2000, 39(12): 2399-2407.
[4]. Kataoka K, Hara K, Haranishi Y, et al. The antinociceptive effect of SNAP5114, a gamma-aminobutyric acid transporter-3 inhibitor, in rat experimental pain models. Anesth Analg, 2013, 116(5): 1162-1169.
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