| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg |
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| Other Sizes |
| Targets |
The primary targets of Ocinaplon are GABAA receptors. It acts as a positive allosteric modulator (PAM) at these receptors, enhancing the inhibitory effects of GABA. It displays modest selectivity for GABAA α1 receptors and partial agonist activity at α2-, α3-, and α5-containing receptors. Its anxiolytic activity is mediated through modulation of GABAergic neurotransmission.
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| ln Vitro |
In vitro, Ocinaplon potentiates GABA-induced currents across α1-, α2-, α3-, and α5-containing GABAA receptor isoforms. It displays modest selectivity for α1-containing receptors. Its activity is typically measured using electrophysiological techniques (e.g., patch-clamp) in cells expressing GABAA receptors or using radioligand binding assays.
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| ln Vivo |
In vivo, Ocinaplon exhibits anxiolytic activity in animal models. It was initially developed as an anxiolytic and muscle relaxant for the treatment of generalized anxiety disorder. Its effects are mediated through modulation of GABAA receptors in the central nervous system.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Ocinaplon involve radioligand binding studies using cell membranes expressing GABAA receptor subtypes. Competitive binding assays are performed using a radiolabeled benzodiazepine or a selective GABAA receptor ligand to determine the compound's affinity for the receptor. Its positive allosteric modulator activity is assessed by measuring its ability to enhance GABA-induced chloride influx in cells expressing GABAA receptors.
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| Cell Assay |
In vitro cellular assays for Ocinaplon are conducted in cell lines expressing GABAA receptors. Cells are treated with the compound, and its effects on GABA-induced currents are measured using electrophysiological techniques such as patch-clamp or two-electrode voltage clamp. Its ability to potentiate GABA responses is quantified by measuring the increase in chloride current amplitude.
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| Animal Protocol |
In vivo animal studies for Ocinaplon are conducted in animal models of anxiety, such as the elevated plus maze, light-dark box, or social interaction test. The compound is administered orally or intraperitoneally, and its anxiolytic-like effects are assessed by measuring behavioral changes. Its muscle relaxant effects can be evaluated using the rotarod test.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Ocinaplon indicate it has a molecular weight of 301.30 and a molecular formula of C17H11N5O. It is a small molecule with good oral bioavailability. Its pharmacokinetics are consistent with those of other benzodiazepine-like compounds. It is typically stored at room temperature.
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| Toxicity/Toxicokinetics |
Toxicological information for Ocinaplon is derived from preclinical and clinical studies. As a GABAA receptor modulator, it may cause sedation, drowsiness, and dependence with long-term use. Its safety profile is similar to that of benzodiazepines. It was discontinued from development for generalized anxiety disorder due to hepatotoxicity concerns.
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| References | |
| Additional Infomation |
Drug Indication
It has been studied for the treatment of anxiety disorders. Ocinaplon is a GABAA receptor modulator that was developed as an anxiolytic. It is also known as DOV 273547. It displays modest selectivity for GABAA α1 receptors and partial agonist activity at other GABAA receptor subtypes. It was discontinued from clinical development due to hepatotoxicity. It is available from research chemical suppliers. |
| Molecular Formula |
C17H11N5O
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|---|---|
| Molecular Weight |
301.309
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| Exact Mass |
301.096
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| CAS # |
96604-21-6
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| PubChem CID |
216456
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.37 g/cm3
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| Index of Refraction |
1.732
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| LogP |
2.417
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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
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| Heavy Atom Count |
23
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| Complexity |
425
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OQJFBUOFGHPMSR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H11N5O/c23-16(14-3-1-2-7-19-14)13-11-21-22-15(6-10-20-17(13)22)12-4-8-18-9-5-12/h1-11H
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| Chemical Name |
pyridin-2-yl-(7-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-3-yl)methanone
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| Synonyms |
CL 273547; CL 273,547; Ocinaplon
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~2 mg/mL (~6.64 mM)
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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 | 3.3188 mL | 16.5942 mL | 33.1884 mL | |
| 5 mM | 0.6638 mL | 3.3188 mL | 6.6377 mL | |
| 10 mM | 0.3319 mL | 1.6594 mL | 3.3188 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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