| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 0.034 μM (the binding of H-GABA)[1]
Piperidine-4-sulfonic acid acts as an agonist at multiple GABAA receptor subunits, including GABRA2, GABRA3, and GABRA5, while also showing antagonist properties at GABRR1, GABRR2, and GABRR3 receptors. This complex interaction pattern makes it a valuable pharmacological tool for dissecting the roles of various GABA receptor subtypes. |
|---|---|
| ln Vitro |
In non-cellular assays using radioligand binding techniques, Piperidine-4-sulfonic acid potently inhibits the binding of H-GABA to its receptor with an IC50 of 0.034 microM. This high potency demonstrates its strong affinity for the GABA binding site, making it a highly effective probe for competitive binding studies at GABA receptors in synaptic membrane preparations.
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| ln Vivo |
Detailed in vivo activity data for Piperidine-4-sulfonic acid is limited, as it is primarily a research tool for in vitro electrophysiology. As a rigid GABA analog, it is expected to produce classical GABAA receptor-mediated effects, such as neuronal hyperpolarization and reduced neuronal excitability, but its specific in vivo pharmacokinetic and pharmacodynamic profile is not the primary focus of its application.
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| Enzyme Assay |
A standard non-cellular protocol involves the inhibition of H-GABA binding. Synaptic membranes are prepared from rat brain homogenates. These membranes are then incubated with 10 nM H-GABA and varying concentrations of Piperidine-4-sulfonic acid (0.1 nM to 10 microM) in Tris-HCl buffer for 30 minutes at 4degC. The reaction is terminated by rapid filtration through glass fiber filters, and the retained radioactivity is measured by scintillation counting to calculate the IC50 for displacement.
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| Cell Assay |
There is no standard cell-based assay for this compound, as its primary mechanism is direct and does not rely on cellular metabolic activity or viability. Instead, its effect is almost exclusively studied in electrophysiological setups using primary neurons or brain slices, where the direct activation of GABAA receptors and subsequent chloride ion flux are measured to determine its potency and efficacy.
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| Animal Protocol |
In vivo animal studies are not typically performed with this compound. As a permanently charged sulfonic acid derivative, it is a highly polar molecule that is not expected to cross the blood-brain barrier efficiently, limiting its utility in whole-animal studies. Therefore, its pharmacological characterization is almost exclusively conducted in vitro using brain tissue preparations or cultured neurons.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for this compound are not well-documented due to its status as a non-drug research tool. Piperidine-4-sulfonic acid contains a sulfonic acid group, which is ionized at physiological pH, making the molecule highly polar. This polarity suggests poor oral bioavailability and limited ability to penetrate cell membranes and the blood-brain barrier, which restricts its use primarily to in vitro applications.
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| Toxicity/Toxicokinetics |
Detailed toxicological studies are not available for this compound. As a tool for in vitro research, it is not developed for clinical use. General laboratory safety precautions should be followed when handling the powder, including the use of gloves and eye protection to avoid direct contact, as its safety profile in humans has not been established beyond its use in controlled research settings.
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| References |
[1]. POVL KROGSGAARD-LARSEN, et al. Pharmacological Studies of Interactions Between Benzodiazepines and GABA Receptors. Brain Research Rullrrin. 1980, 5(2):867-872.
[2]. Krogsgaard-Larsen P, Arnt J. Pharmacological studies of interactions between benzodiazepines and GABA receptors. Brain Research Bulletin, 1980, 5: 867-872. |
| Additional Infomation |
Specific GABA agonists
Piperidine-4-sulfonic acid is a classified as a GABAA agonist and a key research chemical for neuroscience. It is often used as a positive control in experiments designed to discover new GABAergic drugs. Unlike the more flexible GABA molecule, its rigid piperidine ring restricts its conformation, forcing it to adopt only one active shape, which provides researchers with a definitive structural model for drug design targeting GABAA receptors. |
| Molecular Formula |
C5H11NO3S
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|---|---|
| Molecular Weight |
165.21
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| Exact Mass |
165.046
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| CAS # |
72450-62-5
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| PubChem CID |
4838
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| Appearance |
Light brown to brown solid powder
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| Density |
1.39g/cm3
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| Melting Point |
> 300 °C
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| Index of Refraction |
1.537
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| LogP |
1.035
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
10
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| Complexity |
187
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CNCCC1S(=O)(=O)O
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| InChi Key |
UGBJGGRINDTHIH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H11NO3S/c7-10(8,9)5-1-3-6-4-2-5/h5-6H,1-4H2,(H,7,8,9)
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| Chemical Name |
piperidine-4-sulfonic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.0529 mL | 30.2645 mL | 60.5290 mL | |
| 5 mM | 1.2106 mL | 6.0529 mL | 12.1058 mL | |
| 10 mM | 0.6053 mL | 3.0265 mL | 6.0529 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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