| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Panadiplon targets the GABA-A receptor as a partial agonist. It displays selectivity for 5GABAA receptors versus 1GABAA receptors. It modulates GABAergic neurotransmission, which plays a crucial role in anxiety regulation.
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|---|---|
| ln Vitro |
In vitro, panadiplon is a selective GABA receptor agonist and partial agonist of 5GABAA. It displays selectivity for 5GABAA receptors versus 1GABAA receptors. Its activity at the benzodiazepine receptor has been characterized.
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| ln Vivo |
In vivo, panadiplon has been investigated for the treatment of anxiety disorders. It is an anxiolytic compound. It modulates GABAergic neurotransmission.
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| Enzyme Assay |
In vitro receptor binding assays for panadiplon typically use membrane preparations from cells expressing GABA-A receptor subtypes. Radiolabeled benzodiazepine ligands are displaced by increasing concentrations of the compound to determine binding affinity. Functional assays measure the compound's ability to modulate GABA-induced chloride currents.
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| Cell Assay |
Cell-based functional assays for panadiplon involve measuring GABA-A receptor-mediated chloride influx or calcium mobilization in cells expressing the receptor. Cells are treated with the compound and stimulated with GABA. The compound's ability to modulate receptor activity is quantified.
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| Animal Protocol |
In vivo animal studies for panadiplon typically involve administration to animal models of anxiety. Anxiolytic effects are assessed using behavioral tests such as the elevated plus maze, light-dark box, or open field test. The compound's efficacy and selectivity are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of panadiplon are characteristic of small molecule GABA-A receptor modulators. The compound is orally active. It crosses the blood-brain barrier. Metabolism occurs in the liver. Excretion occurs through renal pathways.
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| Toxicity/Toxicokinetics |
The toxicological profile of panadiplon has been evaluated in preclinical studies. The compound is generally well-tolerated. Common side effects include sedation and ataxia. The safety profile is consistent with GABA-A receptor modulators.
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| References | |
| Additional Infomation |
Panadiplon (FG 10571) is a selective GABA receptor agonist and partial agonist of 5GABAA. It was investigated for the treatment of anxiety disorders. It is not currently approved for clinical use. The compound is a valuable research tool for studying GABA-A receptor pharmacology and anxiety.
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| Molecular Formula |
C18H17N5O2
|
|---|---|
| Molecular Weight |
335.367
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| Exact Mass |
335.138
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| CAS # |
124423-84-3
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| PubChem CID |
3033821
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
605.4±65.0 °C at 760 mmHg
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| Flash Point |
319.9±34.3 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.785
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
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| Complexity |
540
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(N1C2=CC=CC=C2N2C=NC(C3=NOC(C4CC4)=N3)=C2C1=O)C
|
| InChi Key |
ZGEGOFCLSWVVKG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17N5O2/c1-10(2)23-13-6-4-3-5-12(13)22-9-19-14(15(22)18(23)24)16-20-17(25-21-16)11-7-8-11/h3-6,9-11H,7-8H2,1-2H3
|
| Chemical Name |
3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-propan-2-ylimidazo[1,5-a]quinoxalin-4-one
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| Synonyms |
FD 10571; FD-10571; Panadiplon
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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 | 2.9818 mL | 14.9089 mL | 29.8178 mL | |
| 5 mM | 0.5964 mL | 2.9818 mL | 5.9636 mL | |
| 10 mM | 0.2982 mL | 1.4909 mL | 2.9818 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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