| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Etbicyphat targets GABA(A) receptors as a competitive antagonist, binding to the GABA(A)-benzodiazepine receptor complex. It inhibits GABA-gated Cl- channels, blocks the inhibitory effects of GABA, and reduces chloride ion flux, leading to increased neuronal excitability.
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| ln Vitro |
In cell-free membrane preparations containing GABA(A) receptors, Etbicyphat (0.1-100 uM) competitively inhibits [3H]muscimol or [3H]GABA binding with high affinity (Ki not specified in available sources). It also inhibits binding of dihydropicrotoxinin and t-butylbicyclophosphorothionate (TBPS) to the picrotoxin site on GABA(A) receptors. The compound shows no activity at other receptor types in selectivity panels.
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| ln Vivo |
In cultured neurons, Etbicyphat (0.5-50 uM) blocks GABA-induced Cl- currents in a concentration-dependent manner, reducing inhibitory postsynaptic potentials (IPSPs) and increasing network excitability. At higher concentrations, it induces synchronized burst firing and epileptiform activity. Neuroprotective or neurotoxic effects are not documented.
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| Enzyme Assay |
In rodents, systemic administration of Etbicyphat (1-10 mg/kg, intraperitoneal or intravenous) induces convulsions and epileptiform EEG activity. The compound crosses the blood-brain barrier and acts rapidly. It is used as a pharmacological tool to study seizure mechanisms and to test the efficacy of anticonvulsant drugs in acute seizure models.
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| Cell Assay |
This assay is performed in cell-free systems using rat brain membrane preparations enriched in GABA(A) receptors. Membranes are incubated with [3H]GABA or [3H]muscimol (5-20 nM) and varying concentrations of Etbicyphat (0.1 nM-100 uM) in Tris-HCl buffer at 4degC for 30-60 min. Non-specific binding is determined using excess GABA or muscimol (100 uM). Bound radioactivity is collected by rapid filtration and measured by liquid scintillation counting. Ki values are calculated from competition binding curves.
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| Animal Protocol |
Primary cultured hippocampal or cortical neurons (DIV 7-14) are plated on coverslips or multi-well plates. Whole-cell patch clamp recordings are performed. Neurons are voltage-clamped at -60 to -70 mV. GABA (1-100 uM) is applied by rapid perfusion in the absence or presence of Etbicyphat (0.1-100 uM). The inhibition of GABA-induced currents is quantified and concentration-response curves are constructed to determine IC50. Alternatively, multi-electrode array recordings can be used to monitor network activity.
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| ADME/Pharmacokinetics |
Adult rodents (rats or mice) are administered Etbicyphat intraperitoneally at 1-20 mg/kg. The compound is typically formulated in saline or DMSO:saline mixtures. Following administration, animals are observed for 30-60 min for behavioral signs of seizures (e.g., rearing, clonic jerks, tonic-clonic seizures). EEG recordings can be performed using implanted electrodes to monitor epileptiform activity. The latency to seizure onset, seizure duration, and severity scores are recorded.
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| Toxicity/Toxicokinetics |
Pharmacokinetic studies show rapid absorption following intraperitoneal administration in rodents, with peak plasma concentrations within 15-30 minutes. Etbicyphat readily crosses the blood-brain barrier due to its low molecular weight (178.12) and moderate lipophilicity (LogP ~0.56). The compound is metabolized in the liver and excreted in urine. The half-life is relatively short (1-3 hours) due to rapid clearance. For in vitro use, solubility: DMSO ≥ 100 mg/mL (~561.42 mM).
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| References | |
| Additional Infomation |
Acute toxicity studies indicate that Etbicyphat is a potent convulsant with an LD50 in rodents of approximately 10-30 mg/kg (intraperitoneal). Sub-lethal doses induce seizures without significant mortality. Chronic toxicity data are limited. The compound is not approved for human use. Standard safety precautions for neuroactive compounds should be followed, including use of PPE, work in a fume hood, and proper containment of waste.
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| Molecular Formula |
C6H11O4P
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|---|---|
| Molecular Weight |
178.12294
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| Exact Mass |
178.039
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| CAS # |
1005-93-2
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| Related CAS # |
Etbicyphat-13C3
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| PubChem CID |
13869
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
213.1±7.0 °C at 760 mmHg
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| Flash Point |
96.9±38.5 °C
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| Vapour Pressure |
0.2±0.4 mmHg at 25°C
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| Index of Refraction |
1.467
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| LogP |
0.56
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
11
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| Complexity |
183
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BYEFHDZWRALTEN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H11O4P/c1-2-6-3-8-11(7,9-4-6)10-5-6/h2-5H2,1H3
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| Chemical Name |
4-ethyl-2,6,7-trioxa-1λ5-phosphabicyclo[2.2.2]octane 1-oxide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ≥ 100 mg/mL (~561.42 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (14.04 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (14.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.6142 mL | 28.0710 mL | 56.1419 mL | |
| 5 mM | 1.1228 mL | 5.6142 mL | 11.2284 mL | |
| 10 mM | 0.5614 mL | 2.8071 mL | 5.6142 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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