| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
CO-102862 targets voltage-gated sodium channels (NaV), which are responsible for the initiation and propagation of action potentials in neurons. It acts as a state-dependent blocker, binding preferentially to the inactivated state of the channel. By blocking sodium channels, it reduces neuronal excitability and prevents the spread of seizure activity.
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| ln Vitro |
In vitro, CO-102862 is a potent blocker of voltage-gated sodium channels. It is a broad-spectrum and state-dependent blocker. Its anticonvulsant activity is attributed to its ability to block sodium channels.
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| ln Vivo |
In vivo, CO-102862 is an orally active anticonvulsant. It has been studied for its potential use in treating epilepsy and other seizure disorders. Its state-dependent blocking mechanism suggests it may have a favorable side-effect profile.
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| Enzyme Assay |
CO-102862 is evaluated in cell-free assays to measure its binding to voltage-gated sodium channels. Radioligand binding displacement assays are performed using membrane preparations expressing sodium channels. Competition binding experiments are conducted with increasing concentrations of CO-102862 and a fixed concentration of a labeled reference ligand.
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| Cell Assay |
CO-102862 is assessed in cell-based electrophysiological assays using neurons or cells expressing voltage-gated sodium channels. The compound's ability to block sodium currents is measured using patch-clamp recordings. Its state-dependent blocking properties are evaluated by measuring block at different membrane potentials.
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| Animal Protocol |
CO-102862 is administered orally in animal models to evaluate its anticonvulsant efficacy. It has been studied in models of epilepsy and other seizure disorders. Efficacy is assessed by measuring seizure threshold, seizure severity, and protection against induced seizures.
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| ADME/Pharmacokinetics |
CO-102862 has a molecular weight of 273.26 and a molecular formula of C14H12FN3O2. It has a CAS number of 181144-66-1. The compound is soluble in DMSO at <27.32 mg/mL. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CO-102862. The compound is for research use only and is not intended for human therapeutic use. It is a potent sodium channel blocker used to study epilepsy and other seizure disorders.
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| References | |
| Additional Infomation |
[[4-(4-fluorophenoxy)phenyl]methyleneamino]urea is an aromatic ether.
CO-102862 is also known as V102862 and Co 102862. It is a highly potent, broad-spectrum, and state-dependent voltage-gated sodium channel blocker. It is an orally active anticonvulsant. The compound is not approved for clinical use. |
| Molecular Formula |
C14H12FN3O2
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|---|---|
| Molecular Weight |
273.26
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| Exact Mass |
273.091
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| CAS # |
181144-66-1
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| PubChem CID |
9816959
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| Appearance |
White to off-white solid powder
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| Density |
1.278g/cm3
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| Index of Refraction |
1.589
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| LogP |
3.711
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
335
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1/C=N/NC(=O)N)OC2=CC=C(C=C2)F
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| InChi Key |
MHUUDVZSPFRUSK-RQZCQDPDSA-N
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| InChi Code |
InChI=1S/C14H12FN3O2/c15-11-3-7-13(8-4-11)20-12-5-1-10(2-6-12)9-17-18-14(16)19/h1-9H,(H3,16,18,19)/b17-9+
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| Chemical Name |
[(E)-[4-(4-fluorophenoxy)phenyl]methylideneamino]urea
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| Synonyms |
CO102862; CO 102862; CO-102862
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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) |
DMSO : ~41.67 mg/mL (~152.49 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 | 3.6595 mL | 18.2976 mL | 36.5952 mL | |
| 5 mM | 0.7319 mL | 3.6595 mL | 7.3190 mL | |
| 10 mM | 0.3660 mL | 1.8298 mL | 3.6595 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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