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(S)-SNAP 5114

Catalog No.GC15464

GABA uptake inhibitor

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(S)-SNAP 5114 Chemical Structure

Cas No.: 157604-55-2

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10mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

(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.

Chemical Properties

Cas No. 157604-55-2 SDF
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
Formula C30H35NO6 M.Wt 505.61
Solubility <25.28mg/ml in ethanol; <50.56mg/ml in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9778 mL 9.889 mL 19.7781 mL
5 mM 0.3956 mL 1.9778 mL 3.9556 mL
10 mM 0.1978 mL 0.9889 mL 1.9778 mL
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