| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
GABAA receptor modulator-10 (Compound 10) (10 μM) enhanced the function of α1β2γ2 GABAA receptor in HEK293T cells overexpressing α1β2γ2 GABAA receptor by MQAE-based fluorescence assay [1]. GABAA receptor modulator-10 (0.1-100 μM) enhanced the GABA-induced current (EC50 = 1.99 μM, Emax = 80.1%) in HEK293T cells overexpressing α1β2γ2 GABAA receptor in a concentration-dependent manner by patch-clamp assay [1].
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| ln Vivo |
GABAA receptor modulator-10 (compound 10) (10 μM, 3 hours before PTZ treatment) reduced the total migration distance of AB zebrafish fertilized 6 days later [1]. GABAA receptor modulator-10 (0.3–30 mg/kg, lateral, 1 hour before PTZ injection) prolonged phase I and III engineering in a schematic model of PTZ manipulation. GABAA receptor modulator-10 (30 mg/kg, orally, 30 minutes before KA injection) induced severity in a KA-induced demonstrative leaf model and reduced the severity of the disease in participants [1].
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| Animal Protocol |
Animal/Disease Models: PTZ-induced mouse epilepsy model: Male KM mice (18-20 g) were were subcutaneously injected with 85 mg/kg PTZ (dissolved in saline) to induce seizures[1]
Doses: 0.3 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: p.o., 1 h before PTZ injection Experimental Results: Prolonged the latency of stage I seizures by 1.21-, 0.96-, 1.53-, and 2.20-fold, and stage III seizures by 1.02-, 1.03-, 1.22-, and 1.45-fold, respectively. Shortened the duration of stage III seizures. Animal/Disease Models: KA-induced mouse temporal lobe epilepsy (TLE) model: Male C57B6/J mice (18-20 g) were intraperitoneally injected with 30 mg/kg kainic acid (KA, dissolved in saline) to induce TLE[1] Doses: 30 mg/kg Route of Administration: p.o., 30 min before KA injection Experimental Results: Attenuated seizure severity. Showed comparable effect to diazepam. |
| References |
| Molecular Formula |
C20H15CLFN5O
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|---|---|
| Molecular Weight |
395.82
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| Appearance |
Typically exists as solids at room temperature
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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 | 2.5264 mL | 12.6320 mL | 25.2640 mL | |
| 5 mM | 0.5053 mL | 2.5264 mL | 5.0528 mL | |
| 10 mM | 0.2526 mL | 1.2632 mL | 2.5264 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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