| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
KD: 0.6 μM (GABAC)[1].
TACA targets GABAA and GABAC receptors. It acts as a potent agonist at both receptor types. The compound activates GABA receptors and is used to study receptor function and pharmacology. |
|---|---|
| ln Vitro |
In cell-free receptor binding assays, TACA demonstrates potent agonist activity at GABAA and GABAC receptors. It displaces radiolabeled GABA from receptor binding sites. The compound's efficacy and potency at these receptors have been characterized in various assay systems. Cellular electrophysiology studies using Xenopus oocytes expressing GABA receptors demonstrate that TACA activates GABAC receptors. The compound has been shown to activate both GABAA and GABAC receptors. Concentration-response relationships have been established in various expression systems.
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| ln Vivo |
TACA may be a substrate for the GABA uptake system because it is a strong competitive inhibitor of GABA uptake in rat brain slices[3].
In vivo, TACA shows a proconvulsant action in the electroconvulsive threshold test in mice. The compound enhances GABAergic transmission, which may possess proconvulsant properties. These findings indicate that GABA receptor agonists can have complex effects on seizure susceptibility. |
| Enzyme Assay |
TACA is a research compound and specific experimental protocols for cell-free receptor binding are not detailed in the available literature. Standard GABAA/GABAC receptor binding assays using membrane preparations and radiolabeled ligands would be applicable. Competition binding experiments determine affinity and selectivity at receptor subtypes.
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| Cell Assay |
Cellular electrophysiology experiments for TACA are conducted using two-electrode voltage clamp in Xenopus oocytes expressing recombinant GABA receptors. Oocytes are injected with cRNA encoding receptor subunits, and currents are measured in response to TACA application. Concentration-response curves are generated to determine EC50 and efficacy values.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TACA have not been extensively characterized. As a small amino acid analog, it may have limited oral bioavailability and blood-brain barrier penetration. The compound's proconvulsant effects in mice confirm central nervous system activity.
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| Toxicity/Toxicokinetics |
Toxicity data for TACA are limited. The compound's proconvulsant action indicates potential neurotoxicity at high doses. Proper handling with appropriate safety precautions is required. The compound is used in research settings at controlled concentrations.
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| References |
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| Additional Infomation |
TACA is a research tool for studying GABAA and GABAC receptor pharmacology. It is used to investigate GABAergic neurotransmission and receptor function. The compound has been used to differentiate GABAC receptor pharmacology from GABAA receptors. It is not approved for clinical use.
|
| Molecular Formula |
C4H7NO2
|
|---|---|
| Molecular Weight |
101.10
|
| Exact Mass |
101.048
|
| CAS # |
38090-53-8
|
| PubChem CID |
5310987
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
1.169 g/cm3
|
| Boiling Point |
300.4ºC at 760 mmHg
|
| Melting Point |
>158°C (lit.)
|
| Flash Point |
135.5ºC
|
| LogP |
0.286
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
7
|
| Complexity |
87.7
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(/C=C/C(=O)O)N
|
| InChi Key |
FMKJUUQOYOHLTF-OWOJBTEDSA-N
|
| InChi Code |
InChI=1S/C4H7NO2/c5-3-1-2-4(6)7/h1-2H,3,5H2,(H,6,7)/b2-1+
|
| Chemical Name |
(E)-4-aminobut-2-enoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O: 20 mg/mL (197.82 mM)
DMSO: < 1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 4 mg/mL (39.56 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 9.8912 mL | 49.4560 mL | 98.9120 mL | |
| 5 mM | 1.9782 mL | 9.8912 mL | 19.7824 mL | |
| 10 mM | 0.9891 mL | 4.9456 mL | 9.8912 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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