NS6180
Based on 1 publication(s) in Google Scholar
NS6180 is a new orally active KCa3.1 channel inhibitor. NS6180 inhibits cloned human KCa3.1 channels with an IC50value of 9 nM. NS6180 can be used for the research of inflammatory bowel disease (IBD) .
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.76%
- No. CAS: 353262-04-1
- Fòrmula: C16H12F3NOS
- Peso molecular:323.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) NS6180
More
Actividad biológica
NS6180 (0.001-1 μM) shows inhibition of human KCa3.1 with an IC50 value of 9.4 nM and a K50 value of 11 1.7 nM, respectively[1].
NS6180 (30 nM, 10 μM) has inhibition that dependent on amino acid residues T250 and V275[1].
NS6180 (1, 10, 100 and 1000 nM; 1 min) shows CCCPreported hyperpolarizations of human erythrocytes[1].
NS6180 (1, 10, 100 and 1000 nM; 1 min) blocks the erythrocyte KCa3.1 channels with IC50 values of 14 nM (human KCa3.1 channels), 15 nM (mouse) and 9 nM (rats), respectively[1].
NS6180 (0-5 μM, 48 h) suppresses rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-g production, while exerting smaller effects on IL-4 and TNF-α and no effect on IL-17 production[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:10 mg/kg
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Administration:i.v., i.p. and oral administration; 10 mg/kg; twice daily or once daily
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Result:Had a plasma half-life of 3.8 h, oral or i.p. administration gave low plasma exposure (Cmax: 186 nM and 33 nM, respectively, after administration of 10 mg/kg).
Chemical Information
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No. CAS 353262-04-1
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Appearance Solid
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Peso molecular 323.34
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Fòrmula C16H12F3NOS
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Color White to off-white
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SMILES
O=C1CSC2=CC=CC=C2N1CC3=CC=CC(C(F)(F)F)=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Mol Immunol
Dextran sodium sulfate potentiates NLRP3 inflammasome activation by modulating the KCa3.1 potassium channel in a mouse model of colitis. [Abstract]2022 Aug;19(8):925-943. PMID: 35799057
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (309.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (7.73 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.
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (596 KB)
- English - EN (596 KB)
- Français - FR (596 KB)
- Deutsch - DE (596 KB)
- Norwegian - NO (596 KB)
- Español - ES (596 KB)
- Swedish - SV (596 KB)
- Italian - IT (596 KB)
- Korean - KR (596 KB)
- Portuguese - PT (596 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0927 mL | 15.4636 mL | 30.9273 mL | 77.3182 mL |
| 5 mM | 0.6185 mL | 3.0927 mL | 6.1855 mL | 15.4636 mL | |
| 10 mM | 0.3093 mL | 1.5464 mL | 3.0927 mL | 7.7318 mL | |
| 15 mM | 0.2062 mL | 1.0309 mL | 2.0618 mL | 5.1545 mL | |
| 20 mM | 0.1546 mL | 0.7732 mL | 1.5464 mL | 3.8659 mL | |
| 25 mM | 0.1237 mL | 0.6185 mL | 1.2371 mL | 3.0927 mL | |
| 30 mM | 0.1031 mL | 0.5155 mL | 1.0309 mL | 2.5773 mL | |
| 40 mM | 0.0773 mL | 0.3866 mL | 0.7732 mL | 1.9330 mL | |
| 50 mM | 0.0619 mL | 0.3093 mL | 0.6185 mL | 1.5464 mL | |
| 60 mM | 0.0515 mL | 0.2577 mL | 0.5155 mL | 1.2886 mL | |
| 80 mM | 0.0387 mL | 0.1933 mL | 0.3866 mL | 0.9665 mL | |
| 100 mM | 0.0309 mL | 0.1546 mL | 0.3093 mL | 0.7732 mL |
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