| Size | Price | Stock | Qty |
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| Targets |
Isoguvacine hydrochloride targets the GABAA receptor, acting as a specific agonist. It binds to the receptor with high affinity (Ki = 55 nM) and activates multiple subunit combinations. By activating the GABAA receptor, it mimics the effects of the inhibitory neurotransmitter GABA, leading to an increase in chloride conductance and neuronal hyperpolarization.
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| ln Vitro |
Isotopic vaccinations are conjugated to mouse forebrain synaptic membrane preparations. This particular binding can be substituted by GABA, muscimol, and bicuculline, but not by picrotoxin or diaminobutyric acid. Kinetic data reveal two binding affinities. The highest amounts of binding are reported in the cerebellum, cortex, and hippocampus [1]. The heterosoma vaccine is conjugated to rat forebrain preparations and has pharmacological characteristics similar to the postsynaptic GABA recognition site: transport into synaptosomal preparations via an uptake system similar to the high-affinity GABA uptake system; recently accumulated heterostomy The vaccine is released in a Ca2+-dependent manner and through heterogeneous exchange with external GABA [2]. The isostoma vaccination at a dose of 50 μM inhibited epileptiform episodes in 2 of 6 organotypic hippocampal slice cultures. Isokou vaccination reduces hypomagnesium-induced epileptiform episodes in a dose-dependent manner [3].
In vitro, Isoguvacine hydrochloride is a potent and specific GABAA receptor agonist. It binds to rat synaptic cortical membranes with a Ki of 55 nM. It activates α1β2γ2S, α2β2γ2S, α3β2γ2S, α5β2γ2S, and ρ1 subunit combinations of the GABAA receptor. It inhibits low magnesium-induced seizure-like events in organotypic hippocampal brain slices in a dose-dependent manner. |
| ln Vivo |
In vivo, Isoguvacine hydrochloride is used in research to study GABAergic neurotransmission. Its ability to suppress seizure-like events in hippocampal slices suggests potential anticonvulsant activity. However, it is not used clinically as a therapeutic agent due to its lack of receptor subtype selectivity and potential for side effects.
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| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays for Isoguvacine hydrochloride typically involve radioligand binding studies. Membranes from rat brain or cells expressing GABAA receptors are incubated with the compound and a radiolabeled antagonist (e.g., [³H]muscimol). The compound's affinity (Ki) is determined by competitive displacement.
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| Cell Assay |
In vitro cell-based assays for Isoguvacine hydrochloride use electrophysiological techniques, such as patch-clamp, to measure the activation of GABAA receptors in recombinant cell lines or neurons. The compound's potency (EC₅₀) and efficacy are determined by measuring the chloride current in response to various concentrations. It can also be used in calcium imaging or other functional assays.
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| Animal Protocol |
In vivo animal studies for Isoguvacine hydrochloride would likely involve administering the compound to animal models of epilepsy or anxiety to assess its anticonvulsant or anxiolytic effects. Its effects on behavior and neuronal activity would be monitored. However, its use as a research tool is more common in ex vivo slice preparations.
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| ADME/Pharmacokinetics |
Isoguvacine hydrochloride has a molecular weight of 163.60 g/mol and a molecular formula of C₆H₁₀ClNO₂. It is a hydrochloride salt. It is soluble in water. As a small, polar molecule, it is expected to be well-absorbed but may have limited brain penetration. Detailed pharmacokinetic data are not widely published.
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| Toxicity/Toxicokinetics |
The toxicity profile of Isoguvacine hydrochloride is not extensively detailed in the provided search results. As a GABAA receptor agonist, high doses could lead to central nervous system depression, respiratory depression, and other adverse effects. It is a research compound and is not intended for human therapeutic use.
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| References |
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| Additional Infomation |
Isoguvacine hydrochloride is a specific GABAA receptor agonist. It binds with high affinity (Ki = 55 nM) and activates multiple GABAA receptor subtypes. It is used in research to study GABAergic signaling and has shown anticonvulsant activity in vitro. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C6H10CLNO2
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|---|---|
| Molecular Weight |
163.6021
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| Exact Mass |
163.04
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| CAS # |
68547-97-7
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| Related CAS # |
64603-90-3 (Parent)
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| PubChem CID |
155107
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| Appearance |
White to light yellow solid powder
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| LogP |
1.121
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
10
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| Complexity |
151
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SUWREQRNTXCCBL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H9NO2.ClH/c8-6(9)5-1-3-7-4-2-5;/h1,7H,2-4H2,(H,8,9);1H
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| Chemical Name |
1,2,3,6-tetrahydropyridine-4-carboxylic acid;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~611.25 mM)
DMSO : ~25 mg/mL (~152.81 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (12.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (12.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (12.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (611.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.1125 mL | 30.5623 mL | 61.1247 mL | |
| 5 mM | 1.2225 mL | 6.1125 mL | 12.2249 mL | |
| 10 mM | 0.6112 mL | 3.0562 mL | 6.1125 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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