| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Kv3 modulator 2 targets Kv3 channels, a family of voltage-gated potassium channels that play a critical role in regulating the excitability of fast-spiking neurons, such as cortical interneurons. These channels are responsible for the fast repolarization of action potentials, enabling high-frequency firing. By modulating Kv3 channel activity, the compound can restore impaired Kv3 channel function and support healthy synaptic communication. It has analgesic activity and is used in the prophylaxis or treatment of related disorders.
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| ln Vitro |
In vitro, Kv3 modulator 2 is a potent modulator of Kv3 channels. It is extracted from patent WO2018109484A1 (compound formula (I)). The compound has analgesic activity and is used in the prophylaxis or treatment of related disorders. Its effects on Kv3 channel activity are typically assessed using electrophysiological techniques, such as patch-clamp recordings, in cells expressing Kv3 channels. Its potency and selectivity make it a valuable tool for studying Kv3 channel biology.
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| ln Vivo |
In vivo, Kv3 modulator 2 has analgesic activity and is used for the prophylaxis or treatment of related disorders. It shows therapeutic potential for treating neurological disorders like schizophrenia, epilepsy, and age-related cognitive decline by restoring impaired Kv3 channel function. Further in vivo studies are needed to fully characterize its efficacy, safety, and pharmacokinetic profile.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, Kv3 modulator 2 is not typically used in direct binding assays, as it is an ion channel modulator. Instead, its activity is assessed using electrophysiological techniques, such as patch-clamp or voltage-clamp recordings, in cells expressing Kv3 channels. The compound is applied at various concentrations, and its effects on channel currents are measured. IC₅0 or EC₅0 values are determined from dose-response curves. Selectivity profiling against other ion channels may be performed.
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| Cell Assay |
For in vitro cellular experiments, Kv3 modulator 2 is tested in neurons or cell lines expressing Kv3 channels. Cells are cultured in appropriate media and treated with various concentrations of the compound. Channel activity is assessed using electrophysiological recordings or membrane potential-sensitive dyes. The compound's effects on neuronal excitability, firing frequency, and synaptic transmission are investigated. Cell viability is monitored.
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| Animal Protocol |
For in vivo animal experiments, Kv3 modulator 2 can be administered to rodents via various routes, including oral gavage, intravenous injection, or intraperitoneal injection. The compound's analgesic activity can be evaluated in pain models, such as the formalin test or von Frey test. Its effects on neurological disorders can be assessed in models of schizophrenia, epilepsy, or cognitive decline. Behavioral tests, such as those measuring seizure activity or cognitive function, are used.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Kv3 modulator 2 are not extensively detailed in the provided references. As a small molecule with a molecular weight of 379.41, it may have reasonable oral bioavailability and tissue distribution, including brain penetration. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies. The compound's metabolism and excretion pathways remain to be fully characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for Kv3 modulator 2 are limited, as it is primarily a research tool. As a Kv3 channel modulator, its toxicity would depend on the importance of Kv3 channels for normal neuronal function. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| Additional Infomation |
Kv3 modulator 2 is a research compound used to study Kv3 channel biology and develop therapies for neurological disorders. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is extracted from patent WO2018109484A1, compound formula (I), and has analgesic activity.
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| Molecular Formula |
C21H21N3O4
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|---|---|
| Molecular Weight |
379.409145116806
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| Exact Mass |
379.153
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| CAS # |
2101321-76-8
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| PubChem CID |
135142328
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| Appearance |
White to off-white solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
652
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC[C@@H]1C(=O)N(C(=O)N1)C2=NC=C(C=C2)OC3=C4C(=C(C=C3)C)OCC45CC5
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| InChi Key |
QRZXUERLZJGJMH-CQSZACIVSA-N
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| InChi Code |
InChI=1S/C21H21N3O4/c1-3-14-19(25)24(20(26)23-14)16-7-5-13(10-22-16)28-15-6-4-12(2)18-17(15)21(8-9-21)11-27-18/h4-7,10,14H,3,8-9,11H2,1-2H3,(H,23,26)/t14-/m1/s1
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| Chemical Name |
(5R)-5-ethyl-3-[5-(7-methylspiro[2H-1-benzofuran-3,1'-cyclopropane]-4-yl)oxypyridin-2-yl]imidazolidine-2,4-dione
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~263.57 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 | 2.6357 mL | 13.1784 mL | 26.3567 mL | |
| 5 mM | 0.5271 mL | 2.6357 mL | 5.2713 mL | |
| 10 mM | 0.2636 mL | 1.3178 mL | 2.6357 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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