(S)-SNAP5114
Based on 1 publication(s) in Google Scholar
(S)-SNAP5114 is a non-covalent murine GABA transporter inhibitor with blood-brain barrier penetration ability, which exhibits significant subtype-selective inhibitory activity against mGAT4 (pIC50=5.71, pKi=4.56), much higher than its effects on mGAT1, mGAT2 and mGAT3. (S)-SNAP5114 elevates extracellular GABA concentrations by blocking the GABA reuptake mechanism, thereby enhancing thalamus-specific GABAergic signaling and exerting potential neuromodulatory effects. (S)-SNAP5114 is widely used in studies related to epilepsy, neuropathic pain, anxiety and depression, and various neurodegenerative diseases.
For research use only. We do not sell to patients.
- Purity: 98.09%
- CAS No.: 157604-55-2
- Formula: C30H35NO6
- Molecular Weight:505.60
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) (S)-SNAP5114
More
Biological Activity
IC50: 5 μM (hGAT-3), 21 μM (rGAT-2)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.12 μM
Compound: 7, (S)-SNAP-5114
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Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
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[PMID: 23886812] |
| CHO | IC50 |
11.9 μM
Compound: 7, (S)-SNAP-5114
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Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
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[PMID: 23886812] |
| CHO | IC50 |
170 μM
Compound: 7, (S)-SNAP-5114
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Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
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[PMID: 23886812] |
| CHO | IC50 |
71.7 μM
Compound: 7, (S)-SNAP-5114
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Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
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[PMID: 23886812] |
| CHO | IC50 |
>100 μM
Compound: SNAP5114
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Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
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[PMID: 25147609] |
| CHO | IC50 |
1.12 μM
Compound: SNAP5114
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Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
|
[PMID: 25147609] |
| CHO | IC50 |
11.9 μM
Compound: SNAP5114
|
Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
|
[PMID: 25147609] |
| CHO | IC50 |
71.7 μM
Compound: SNAP5114
|
Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
|
[PMID: 25147609] |
| HEK293 | IC50 |
22 μM
Compound: 7, (S)-SNAP-5114
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Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells
Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells
|
[PMID: 21353350] |
| HEK293 | IC50 |
3 μM
Compound: 7, (S)-SNAP-5114
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Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in human HEK cells
Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in human HEK cells
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[PMID: 21353350] |
| HEK293 | IC50 |
35 μM
Compound: 7, (S)-SNAP-5114
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Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells
Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells
|
[PMID: 21353350] |
| HEK293 | IC50 |
85 μM
Compound: 7, (S)-SNAP-5114
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Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells
Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells
|
[PMID: 21353350] |
| HEK293 | IC50 |
>30 μM
Compound: (S)-1b, SNAP 5114
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Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
|
[PMID: 25882526] |
| HEK293 | IC50 |
20 μM
Compound: (S)-1b, SNAP 5114
|
Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
|
[PMID: 25882526] |
| HEK293 | IC50 |
22 μM
Compound: (S)-1b, SNAP 5114
|
Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
|
[PMID: 25882526] |
| HEK293 | IC50 |
6 μM
Compound: (S)-1b, SNAP 5114
|
Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
|
[PMID: 25882526] |
| HEK293 | IC50 |
199 μM
Compound: 23
|
Inhibition of mouse GAT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
Inhibition of mouse GAT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
|
[PMID: 26706177] |
| HEK293 | IC50 |
21.9 μM
Compound: 23
|
Inhibition of mouse GAT2 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
Inhibition of mouse GAT2 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
|
[PMID: 26706177] |
| HEK293 | IC50 |
6.3 μM
Compound: 23
|
Inhibition of mouse GAT3 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
Inhibition of mouse GAT3 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
|
[PMID: 26706177] |
| HEK293 | IC50 |
>1000 μM
Compound: 23
|
Inhibition of mouse BGT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
Inhibition of mouse BGT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
|
[PMID: 26706177] |
(S)-SNAP-5114 (with 25 min pre-incubation) inhibits [3H]GABA uptake in HEK293 cells expressing mGAT1, mGAT3 and mGAT4, with pIC50 values of 4.07, 5.29 and 5.71, respectively; it only exhibits weak inhibitory activity against mGAT2 at a concentration of 100 μM[1].
(S)-SNAP5114 exhibits poor chemical stability in acidic media, with a half-life of approximately 4 h at pH 4.5[3].
The calculated log D value of (S)-SNAP5114 at pH 7.4 is close to 2, suggesting its potential blood-brain barrier penetration property[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 157604-55-2
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Appearance Solid
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Molecular Weight 505.60
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Formula C30H35NO6
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Color White to off-white
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SMILES
O=C([C@@H]1CN(CCOC(C2=CC=C(OC)C=C2)(C3=CC=C(OC)C=C3)C4=CC=C(OC)C=C4)CCC1)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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iScience
Synaptic scaling of corticostriatal circuits underlies hyperactivity in GABA Transporter-1 deficient mice. [Abstract]2023 Mar 3;26(4):106322. PMID: 36968092
Solvent & Solubility
DMSO : 200 mg/mL (395.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (9.89 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (9.89 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Böck MC, et al. N-Substituted Nipecotic Acids as (S)-SNAP-5114 Analogues with Modified Lipophilic Domains. ChemMedChem. 2020;15(9):756-771. [Content Brief]
[3]. Pabel J, 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9778 mL | 9.8892 mL | 19.7785 mL | 49.4462 mL |
| 5 mM | 0.3956 mL | 1.9778 mL | 3.9557 mL | 9.8892 mL | |
| 10 mM | 0.1978 mL | 0.9889 mL | 1.9778 mL | 4.9446 mL | |
| 15 mM | 0.1319 mL | 0.6593 mL | 1.3186 mL | 3.2964 mL | |
| 20 mM | 0.0989 mL | 0.4945 mL | 0.9889 mL | 2.4723 mL | |
| 25 mM | 0.0791 mL | 0.3956 mL | 0.7911 mL | 1.9778 mL | |
| 30 mM | 0.0659 mL | 0.3296 mL | 0.6593 mL | 1.6482 mL | |
| 40 mM | 0.0494 mL | 0.2472 mL | 0.4945 mL | 1.2362 mL | |
| 50 mM | 0.0396 mL | 0.1978 mL | 0.3956 mL | 0.9889 mL | |
| 60 mM | 0.0330 mL | 0.1648 mL | 0.3296 mL | 0.8241 mL | |
| 80 mM | 0.0247 mL | 0.1236 mL | 0.2472 mL | 0.6181 mL | |
| 100 mM | 0.0198 mL | 0.0989 mL | 0.1978 mL | 0.4945 mL |