| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Kv2-IN-A1 targets the voltage-gated potassium channels Kv2.1 and Kv2.2. It acts as a selective inhibitor (antagonist) of these channels, with IC50 values of 0.2 µM for Kv2.1 and 0.41 µM for Kv2.2. The compound shows good selectivity for Kv2.1 and Kv2.2 over Kv1.2 (IC50 >10 µM) and is more than 10-fold selective over NaV channels and other KV channels. By inhibiting Kv2 channels, Kv2-IN-A1 modulates neuronal excitability and action potential firing.
|
|---|---|
| ln Vitro |
In insulinoma INS-1 cells, KV2 channel inhibitor-1 (compound A1; 0.3, 1, 3 μM; 0-3000s) suppresses KV currents. INS-1 KV current varies by an average of 71% at 0.3 μM and boils by an average of 84% at 3 μM when KV2 channel inhibitor-1 is present [1].
In vitro, Kv2-IN-A1 inhibits Kv2.1 and Kv2.2 channel activity in a concentration-dependent manner. The compound's inhibitory activity has been characterized in electrophysiological assays using cells expressing recombinant Kv2 channels. Kv2-IN-A1 shows potent inhibition of Kv2.1-mediated currents, with an IC50 of 0.2 µM, and Kv2.2-mediated currents, with an IC50 of 0.41 µM. The compound's selectivity for Kv2 channels over other potassium and sodium channels has been confirmed in patch-clamp studies. |
| ln Vivo |
In vivo, Kv2-IN-A1 has been studied in animal models of neurological disorders, including epilepsy. By inhibiting Kv2 channels, the compound modulates neuronal excitability and may reduce seizure activity. However, specific in vivo efficacy data are limited in the available literature, as Kv2-IN-A1 is primarily a research tool for studying Kv2 channel function. The compound is expected to have central nervous system activity due to its ability to cross the blood-brain barrier.
|
| Enzyme Assay |
The non-cellular assay for Kv2-IN-A1 involves measuring its binding affinity for Kv2 channels using radioligand binding assays or its inhibitory activity using automated patch-clamp systems. In a typical electrophysiological assay, cells expressing recombinant Kv2.1 or Kv2.2 channels are patch-clamped, and the inhibition of potassium currents by Kv2-IN-A1 is measured at various concentrations. The IC50 is determined from concentration-response curves.
|
| Cell Assay |
The cellular assay for Kv2-IN-A1 involves treating cells expressing Kv2 channels with the compound and measuring potassium currents using patch-clamp electrophysiology. Cultured neurons or heterologous expression systems (e.g., CHO or HEK293 cells) are used. Cells are treated with Kv2-IN-A1 at various concentrations, and the voltage-dependent potassium currents are recorded. The inhibition of current amplitude is calculated, and the IC50 is determined.
|
| Animal Protocol |
In vivo animal studies for Kv2-IN-A1 typically use rodent models of epilepsy or other neurological disorders. The compound is administered by intraperitoneal injection or oral gavage, and seizure activity is monitored by electroencephalography (EEG) or behavioral observation. However, specific published protocols for Kv2-IN-A1 are limited, as the compound is primarily used in vitro.
|
| ADME/Pharmacokinetics |
Kv2-IN-A1 has a molecular weight of 396.89 and a molecular formula of C₂₀H₁₇ClN₄OS. The compound is soluble in DMSO. It should be stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 1 year. The compound has limited aqueous solubility, with a maximum solubility of approximately 3.97 mg/mL in DMSO.
|
| Toxicity/Toxicokinetics |
The toxicological profile of Kv2-IN-A1 has not been extensively characterized in the published literature. As a potassium channel inhibitor, it may affect cardiac and neuronal excitability at high doses. The compound should be handled with appropriate laboratory safety precautions. Comprehensive toxicity data are limited, as Kv2-IN-A1 is a research compound and not approved for clinical use.
|
| References | |
| Additional Infomation |
Kv2-IN-A1 is a selective inhibitor of Kv2.1 and Kv2.2 voltage-gated potassium channels. It is a valuable research tool for studying the role of Kv2 channels in neuronal excitability, epilepsy, and other neurological disorders. The compound's selectivity for Kv2 channels over other ion channels makes it useful for dissecting the specific contributions of Kv2 channels to cellular electrophysiology. Kv2-IN-A1 is not approved for clinical use and is strictly for research purposes.
|
| Molecular Formula |
C20H17CLN4OS
|
|---|---|
| Molecular Weight |
396.893181562424
|
| Exact Mass |
396.081
|
| Elemental Analysis |
C, 60.53; H, 4.32; Cl, 8.93; N, 14.12; O, 4.03; S, 8.08
|
| CAS # |
689297-68-5
|
| Related CAS # |
689297-68-5;
|
| PubChem CID |
10023694
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.5
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
27
|
| Complexity |
524
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
MRQZOINSVKHDQS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H17ClN4OS/c1-12(13-3-2-4-14(21)8-13)7-19(26)23-15-5-6-16-17(9-15)25-20(24-16)18-10-27-11-22-18/h2-6,8-12H,7H2,1H3,(H,23,26)(H,24,25)
|
| Chemical Name |
3-(3-chlorophenyl)-N-[2-(1,3-thiazol-4-yl)-3H-benzimidazol-5-yl]butanamide
|
| Synonyms |
Kv2INA1; Kv2 IN A1; Kv2-IN-A1
|
| HS Tariff Code |
2934.99.03.00
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~629.90 mM)
|
|---|---|
| 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 | 2.5196 mL | 12.5979 mL | 25.1959 mL | |
| 5 mM | 0.5039 mL | 2.5196 mL | 5.0392 mL | |
| 10 mM | 0.2520 mL | 1.2598 mL | 2.5196 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
