SKA-31
Based on 5 publication(s) in Google Scholar
SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure.
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- 純度: 99.66%
- CAS 番号: 40172-65-4
- 分子式: C11H8N2S
- 分子量:200.27
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Neuroprotective Compound Library
HY-L070
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Potassium Channel Compound Library
HY-L119
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Human Metabolite Library
HY-L123
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Anti-Pulmonary Fibrosis Compound Library
HY-L125
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Heterocyclic Compound Library
HY-L138
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Ion Channel Compound Library
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
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Bioactive Compound Library
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High-Throughput Bioactive Compound Library
HY-L205
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Mass Spectrometry Human Metabolite Library
HY-L215
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MCE Kinase Hinge Binder Fragment Library
HY-L907
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Membrane Transporter/Ion Channel Compound Library
HY-L011
生物活性
EC50: 2.9 μM (KCa2.1), 1.9 μM (KCa2.2), 2.9 μM (KCa2.3), 260 nM (KCa3.1)[1]
SKA-31 activates KCa2/3 channels more potently than PK 26124, and is more selective over other Ion channels[1].
SKA-31 reduces cell viability with IC50s of 5.3 μM , 46.9 μM in HCT-116 cells and HCT-8 cells, respectively[2].
SKA-31 (5.3 μM; 0-96 hours) reduces HCT-116 cells proliferation[2].
SKA-31 triggers apoptosis in HCT-116 cells at 5 μM, and the effect is smaller in HCT-8 cells at 45 μM[2].
SKA-31 increases the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines at 5 μM and 45 μM, respectively[2].
SKA-31 further activates Caspase 3 and reduces Akt phosphorylation induced by CDDP[2].
SKA-31 has a synergic effect with CDDP also on the inhibition of HCT-116 cell proliferation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 cells, HCT-8 cells
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Concentration:
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Incubation Time:24 hours
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Result:Reduced cell viability with IC50s of 5.3 μM , 46.9 μM in HCT-116 and HCT-8, respectively.
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Cell Line:HCT-116 cells
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Concentration:5.3 μM
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Incubation Time:0-96 hours
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Result:Reduced HCT-116 cells proliferation when added at time zero at IC50S value.
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Cell Line:HCT-116 cells, HCT-8 cells
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Concentration:5 μM (HCT-116 cells), 45 μM (HCT-8 cells)
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Incubation Time:24 hours
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Result:Triggered apoptosis in HCT-116 cells, and the effect was smaller in HCT-8 cells.
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Cell Line:HCT-116 cells, HCT-8 cells
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Concentration:5 μM (HCT-116), 45 μM (HCT-8)
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Incubation Time:24 hours
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Result:Increased the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines.
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Cell Line:HCT-116 cells
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Concentration:
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Incubation Time:24 hours
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Result:Further activated Caspase 3 and reduced Akt phosphorylation when co-treatment with CDDP in HCT-116 cells.
SKA-31 potentiates native KCa3.1 and KCa2.3 in murine carotid endothelium with EC50 values of 225 nM and 1.6 μM for KCa3.1 and KCa2.3, respectively[1].
SKA-31 stimulates KCa3.1 and KCa2.3 in vascular endothelial cells and increases acetylcholine-induced endothelium-derived hyperpolarizing factor (EDHF) -mediated vasodilation[1].
SKA-31 potentiates EDHF-type vasodilations and lowers blood pressure in mice. Injections of SKA-31 (1-30 mg/kg; i.p.) lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:16-25 weeks mice[1]
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Dosage:1 mg/kg, 10 mg/kg, and 30 mg/kg
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Administration:Intraperitoneal injection
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Result:Lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).
化学情報
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CAS 番号 40172-65-4
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性状 Solid
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分子量 200.27
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分子式 C11H8N2S
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Color Gray to brown
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SMILES
NC1=NC2=C3C=CC=CC3=CC=C2S1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Life Sci
Regulatory role of Piezo1 channel in endothelium-dependent hyperpolarization-mediated vasorelaxation of small resistance vessels and its anti-inflammatory action. [Abstract]2024 Jan 1:336:122326. PMID: 38056769 -
Eur J Pharmacol
Novel mechanisms of metformin-induced vasorelaxation of mesenteric arterioles via endothelium-dependent hyperpolarization to treat murine colitis. [Abstract]2025 Sep 15:1003:177900. PMID: 40617384 -
Cell Calcium
Drug repurposing DMSO from an old solvent to a new candidate for the treatment of colitis and sepsis in male mice. [Abstract]2026 May 23:136:103155. PMID: 42235215 -
Front Physiol
Cyclopiazonic Acid-Induced Ca2+ Store Depletion Initiates Endothelium-Dependent Hyperpolarization-Mediated Vasorelaxation of Mesenteric Arteries in Healthy and Colitis Mice. [Abstract]2021 Mar 9:12:639857. PMID: 33767636 -
Heliyon
N,N,N',N'-Tetrakis(2-pyridylmethyl)ethylenediamine induces endothelium-dependent hyperpolarization-mediated vasorelaxation via store-operated calcium entry mechanism in healthy and intestinal inflammatory mice. [Abstract]2024 Jul 6;10(14):e33994. PMID: 39108891
溶剤 & 溶解度
DMSO : 125 mg/mL (624.17 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (12.48 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (10.39 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
純度とドキュメンテーション
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データシート (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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- Español - ES (393 KB)
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- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Sankaranarayanan A, et al. Naphtho[1,2-d]thiazol-2-ylamine (SKA-31), a new activator of KCa2 and KCa3.1 potassium channels, potentiates the endothelium-derived hyperpolarizing factor response and lowers blood pressure. Mol Pharmacol. 2009 Feb;75(2):281-95. [Content Brief]
[2]. Serena Pillozzi, et al. The combined activation of KCa3.1 and inhibition of Kv11.1/hERG1 currents contribute to overcome CDDP resistance in colorectal cancer cells. Br J Cancer. 2018 Jan; 118(2): 200–212. [Content Brief]
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.9934 mL | 24.9668 mL | 49.9336 mL | 124.8340 mL |
| 5 mM | 0.9987 mL | 4.9934 mL | 9.9867 mL | 24.9668 mL | |
| 10 mM | 0.4993 mL | 2.4967 mL | 4.9934 mL | 12.4834 mL | |
| 15 mM | 0.3329 mL | 1.6645 mL | 3.3289 mL | 8.3223 mL | |
| 20 mM | 0.2497 mL | 1.2483 mL | 2.4967 mL | 6.2417 mL | |
| 25 mM | 0.1997 mL | 0.9987 mL | 1.9973 mL | 4.9934 mL | |
| 30 mM | 0.1664 mL | 0.8322 mL | 1.6645 mL | 4.1611 mL | |
| 40 mM | 0.1248 mL | 0.6242 mL | 1.2483 mL | 3.1208 mL | |
| 50 mM | 0.0999 mL | 0.4993 mL | 0.9987 mL | 2.4967 mL | |
| 60 mM | 0.0832 mL | 0.4161 mL | 0.8322 mL | 2.0806 mL | |
| 80 mM | 0.0624 mL | 0.3121 mL | 0.6242 mL | 1.5604 mL | |
| 100 mM | 0.0499 mL | 0.2497 mL | 0.4993 mL | 1.2483 mL |
SKA-31 関連分類
HY-111655 関連分類
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