Kv2.1-IN-1
Based on 1 publication(s) in Google Scholar
Kv2.1-IN-1 is an orally active and blood-brain barrier penetrant Kv2.1 inhibitor with an IC50 of 0.07 μM. Kv2.1-IN-1 exhibits a selectivity >130 fold over other K+, Na+, and Ca2+ ion channels. Kv2.1-IN-1 decreases the apoptosis of HEK293 cells induced by H2O2. Kv2.1-IN-1 produces significant neuroprotection efficacy in middle cerebral artery occlusion (MCAO) rat. Kv2.1-IN-1 can be used for the study of ischemic stroke.
For research use only. We do not sell to patients.
- Purity: 98.64%
- CAS No.: 2252448-93-2
- Formula: C22H29N3O3
- Molecular Weight:383.48
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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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Kv2.1-IN-1
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Biological Activity
Kv2.1-IN-1 (0.3-3 mg/kg, i.v. and 5 mg/kg, p.o., single dose) shows anticerebral infarct efficacy in MCAO rats model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MCAO model established in male Sprague−Dawley (SD) rats[1]
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Dosage:0.3, 1 and 3 mg/kg, i.v. and 5 mg/kg, p.o.
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Administration:Intravenous injection (i.v.) or oral administration (p.o.), single dose
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Result:Significantly reduced the infarct volume at the dose of 1 and 3 mg/kg (i.v.) and decrease the cerebral infarction volume ratio and the behavior score noticeably at the dose of 5 mg/kg (p.o.).
Chemical Information
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CAS No. 2252448-93-2
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Appearance Solid
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Molecular Weight 383.48
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Formula C22H29N3O3
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Color White to off-white
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SMILES
O=C(C1=CC(NC(C(C)C)=O)=CC=C1OCC)NC(C2=CC=CC(NC)=C2)C
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Glabridin as a selective Kv2.1 inhibitor ameliorates DPN pathology by disrupting the Aβ/Kv2.1/JNK/NF-κB/NLRP3/p-Tau pathway. [Abstract]2025 Aug;46(8):2163-2179. PMID: 40113986
Solvent & Solubility
DMSO : 100 mg/mL (260.77 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)
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: ≥ 5 mg/mL (13.04 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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 (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 2.6077 mL | 13.0385 mL | 26.0770 mL | 65.1924 mL |
| 5 mM | 0.5215 mL | 2.6077 mL | 5.2154 mL | 13.0385 mL | |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6077 mL | 6.5192 mL | |
| 15 mM | 0.1738 mL | 0.8692 mL | 1.7385 mL | 4.3462 mL | |
| 20 mM | 0.1304 mL | 0.6519 mL | 1.3038 mL | 3.2596 mL | |
| 25 mM | 0.1043 mL | 0.5215 mL | 1.0431 mL | 2.6077 mL | |
| 30 mM | 0.0869 mL | 0.4346 mL | 0.8692 mL | 2.1731 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6519 mL | 1.6298 mL | |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5215 mL | 1.3038 mL | |
| 60 mM | 0.0435 mL | 0.2173 mL | 0.4346 mL | 1.0865 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8149 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6519 mL |
Kv2.1-IN-1 Related Classifications
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