(S)-SNAP 5114 |
| Catalog No.GC15464 |
(S)-SNAP 5114 es un inhibidor selectivo del transporte de GABA, con valores de IC50 de 5 μM y 21 μM para hGAT-3 y rGAT-2, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 157604-55-2
Sample solution is provided at 25 µL, 10mM.
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(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.
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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