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(S)-SNAP 5114
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
(S)-SNAP 5114图片
CAS NO:157604-55-2
包装与价格：
包装价格(元)
50mg电议
10mg电议

产品介绍
(S)-SNAP 5114 是一种选择性 GABA 转运抑制剂，对 hGAT-3 和 rGAT-2 的 IC50 值分别为 5 μM 和 21 μM。
Cas No.157604-55-2
化学名(S)-1-(2-(tris(4-methoxyphenyl)methoxy)ethyl)piperidine-3-carboxylic acid
Canonical SMILESOC([C@@H]1CN(CCOC(C(C=C2)=CC=C2OC)(C(C=C3)=CC=C3OC)C(C=C4)=CC=C4OC)CCC1)=O
分子式C30H35NO6
分子量505.61
溶解度<25.28mg/ml in ethanol;<50.56mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

(S)-SNAP 5114 is a selective inhibitor of GABA transport with IC50 values of 5, 21 and 388 μM for hGAT-3, rGAT-2 and hGAT-1, respectively [1].

γ-Aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the central nervous system (CNS) and plays a critical role in Huntington’s disease, Parkinson’s disease, epilepsy, schizophrenia and Alzheimer’s disease. GABA transporters transport GABA from extra- to intracellular side of glial and neuronal cells [2].

(S)-SNAP 5114 is a selective GABA transport inhibitor. In HEK-293 cell lines expressing mGAT1-4, (S)-SNAP 5114 exhibited inhibitory potencies with pIC50 values of 4.07, 5.29 and 5.71 for mGAT1, mGAT3 and mGAT4 respectively and inhibited mGAT2 by 56% [2]. SNAP-5114 (100 μM) increased GABA levels to 247% in the thalamus. In juvenile rats with maximal electroshock, SNAP-5114 inhibited tonic hindlimb extension. In DBA/2 mice, SNAP-5114 inhibited sound induced convulsions in a dose-dependent way with ED50 value of 110 μmol/kg [3]. In rats, SNAP5114 (10, 50, 100 or 200 μg) inhibited the late-phase response in the formalin test and prolonged withdrawal latencies in the tail flick test, which suggested that SNAP5114 inhibited chemical and thermal nociception. In the chronic constriction injury rats, SNAP5114 inhibited mechanical allodynia in a dose-dependent way [4].

References:
[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.