| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
The primary target is the GABA receptor system, with a unique GABAergic mechanism distinct from benzodiazepines and barbiturates. At 30 μM, DSP-0565 shows no binding to flunitrazepam, muscimol, Ro-15-1788, TBOB, or TBPS binding sites, indicating a novel target within the GABAergic system. It acts as a broad-spectrum anti-epileptic agent with a unique mechanism of action.
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|---|---|
| ln Vitro |
In vitro, DSP-0565 shows anti-convulsant activity in various models with good safety margin. It exhibits a unique GABAergic function that differs from classical GABA-A receptor modulators. The compound does not bind to conventional benzodiazepine, GABA, or picrotoxin sites at 30 μM, suggesting it operates through a novel target. It is used as a research tool for studying GABAergic mechanisms in epilepsy.
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| ln Vivo |
In vivo, DSP-0565 demonstrates anti-convulsant activity in various animal models, including subcutaneous pentylenetetrazole (scPTZ), maximal electroshock (MES), 6 Hz psychomotor seizure, and amygdala kindling models. It shows a broad-spectrum anti-epileptic profile with a good safety margin. The compound is used as a tool for evaluating novel anti-epileptic drug candidates in preclinical models.
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| Enzyme Assay |
For non-cellular binding assays, DSP-0565 at 30 μM is tested for binding to flunitrazepam, muscimol, Ro-15-1788, TBOB, and TBPS binding sites using radioligand binding assays with rat brain membranes. No significant binding to these conventional GABA-A receptor sites is observed, indicating a novel mechanism of action.
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| Cell Assay |
For cell-based assays, DSP-0565 is tested for its effects on GABA-induced currents using patch-clamp electrophysiology in cultured neurons or recombinant GABA-A receptors expressed in HEK293 cells. Its unique GABAergic function is assessed by measuring modulation of GABA-evoked chloride currents at various concentrations.
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| Animal Protocol |
For in vivo experiments, DSP-0565 is administered to rodents via intraperitoneal or oral routes in various seizure models. In the scPTZ model, mice are injected with pentylenetetrazole, and the latency to clonic seizures is measured. In the MES model, maximal electroshock is applied, and tonic hindlimb extension is assessed. In the 6 Hz model, corneal stimulation is applied, and seizure protection is evaluated.
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| References |
| Molecular Formula |
C14H12FNO
|
|---|---|
| Molecular Weight |
229.249587059021
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| Exact Mass |
229.09
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| CAS # |
1226855-28-2
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| PubChem CID |
46189864
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
269
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C(=C1)CC(=O)N)C2=CC=CC=C2F
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| InChi Key |
MWAPNZXZUGCADE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H12FNO/c15-13-8-4-3-7-12(13)11-6-2-1-5-10(11)9-14(16)17/h1-8H,9H2,(H2,16,17)
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| Chemical Name |
2-[2-(2-fluorophenyl)phenyl]acetamide
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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 | 4.3621 mL | 21.8103 mL | 43.6205 mL | |
| 5 mM | 0.8724 mL | 4.3621 mL | 8.7241 mL | |
| 10 mM | 0.4362 mL | 2.1810 mL | 4.3621 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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