KV2 channel inhibitor-1
Based on 1 Customer Validation
KV2 channel inhibitor-1 is a selective KV2 channel inhibitor with IC50s of 0.2 μM and 0.41 μM for KV2.1 and KV2.2, respectively. KV2 channel inhibitor-1 possesses good selectivity over KV1.2 (IC50>10 μM). KV2 channel inhibitor-1 is >10-fold selective over NaV channels and other KV channels and displays weak activity on CaV channels.
For research use only. We do not sell to patients.
- Purity : 98.75%
- CAS No.: 689297-68-5
- Formula: C20H17ClN4OS
- Molecular Weight:396.89
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
IC50: 0.2 μM (KV2.1), 0.41 μM (KV2.2), 12.1 μM (KV1.2), 9.5 μM (KV1.5), >20 μM (KV3.2), 2.9 μM (KV11.1), 6.6 μM (CaV1.2), >10 μM (CaV2.1), >10 μM (CaV2.2), 5.7 μM (CaV2.3), >10 μM (NaV1.5), 8 μM (NaV1.7)[1]
In Vitro
KV2 channel inhibitor-1 (compound A1; 0.3, 1, 3 μM; 0-3000s) inhibits the KV current in rat insulinoma INS-1 cells. KV2 channel inhibitor-1 blocks INS-1 KV current an average of 71% at 0.3 μM and 84% at 3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 689297-68-5
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Appearance Solid
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Molecular Weight 396.89
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Formula C20H17ClN4OS
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Color White to off-white
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SMILES
O=C(NC1=CC=C2N=C(C3=CSC=N3)NC2=C1)CC(C)C4=CC=CC(Cl)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (251.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5196 mL | 12.5979 mL | 25.1959 mL | 62.9897 mL |
| 5 mM | 0.5039 mL | 2.5196 mL | 5.0392 mL | 12.5979 mL | |
| 10 mM | 0.2520 mL | 1.2598 mL | 2.5196 mL | 6.2990 mL | |
| 15 mM | 0.1680 mL | 0.8399 mL | 1.6797 mL | 4.1993 mL | |
| 20 mM | 0.1260 mL | 0.6299 mL | 1.2598 mL | 3.1495 mL | |
| 25 mM | 0.1008 mL | 0.5039 mL | 1.0078 mL | 2.5196 mL | |
| 30 mM | 0.0840 mL | 0.4199 mL | 0.8399 mL | 2.0997 mL | |
| 40 mM | 0.0630 mL | 0.3149 mL | 0.6299 mL | 1.5747 mL | |
| 50 mM | 0.0504 mL | 0.2520 mL | 0.5039 mL | 1.2598 mL | |
| 60 mM | 0.0420 mL | 0.2100 mL | 0.4199 mL | 1.0498 mL | |
| 80 mM | 0.0315 mL | 0.1575 mL | 0.3149 mL | 0.7874 mL | |
| 100 mM | 0.0252 mL | 0.1260 mL | 0.2520 mL | 0.6299 mL |
KV2 channel inhibitor-1 Related Classifications
HY-44153 Related Classifications
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