S3969
Based on 1 Customer Validation
S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). The apparent EC50 for S3969 activation of hENaC is 1.2 μm.
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- Pureté: 99.15%
- CAS No.: 1027997-01-8
- Formule: C17H24N2O2S
- Masse moléculaire:320.45
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Stockage:Powder -20°C, 3 years , 4°C, 2 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
S3969 fully and reversibly activates hENaC in heterologous cells. S3969 activates δβγ, αβγ, α2βγ, δ2βγ, and αβG37Sγ hENaC with EC50s of 1.2±0.2 μM, 1.2±0.1 μM, 1.2±0.5, 0.4±0.1,and 1.2±0.4 μM[1].
S3969 does not activate αβγ mouse ENaC (mENaC) at concentrations yielding maximal activation of αβγ hENaC or δβγ hENaC. Weak αβγ mENaC activation was observed at high concentrations of S3969 (100-300 μm)[1].
S3969 exhibits high efficacy (600-700% hENaC activation at 30 μm) as well as potency on wild-type hENaC (apparent EC50 ∼1 μm for αβγ hENaC and δβγ hENaC but not αβγ mENaC) [1].
ENaC-activator S3969 (10 µM) stimulates αF61L mutant ENaC more than wild-type ENaC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1027997-01-8
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Appearance Solid
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Masse moléculaire 320.45
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Formule C17H24N2O2S
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Color Off-white to light yellow
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SMILES
CC(C)CC(SC1=CNC2=C1C(C)=CC=C2)C(NCCO)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (312.06 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 (7.80 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: ≥ 2.5 mg/mL (7.80 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 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.
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.
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
[1]. Min Lu, et al. Small molecule activator of the human epithelial sodium channel. J Biol Chem. 2008 May 2;283(18):11981-94. [Content Brief]
[2]. Regina Huber, et al. Functional characterization of a partial loss-of-function mutation of the epithelial sodium channel (ENaC) associated with atypical cystic fibrosis. Cell Physiol Biochem. 2010;25(1):145-58. [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 |
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| DMSO | 1 mM | 3.1206 mL | 15.6031 mL | 31.2061 mL | 78.0153 mL |
| 5 mM | 0.6241 mL | 3.1206 mL | 6.2412 mL | 15.6031 mL | |
| 10 mM | 0.3121 mL | 1.5603 mL | 3.1206 mL | 7.8015 mL | |
| 15 mM | 0.2080 mL | 1.0402 mL | 2.0804 mL | 5.2010 mL | |
| 20 mM | 0.1560 mL | 0.7802 mL | 1.5603 mL | 3.9008 mL | |
| 25 mM | 0.1248 mL | 0.6241 mL | 1.2482 mL | 3.1206 mL | |
| 30 mM | 0.1040 mL | 0.5201 mL | 1.0402 mL | 2.6005 mL | |
| 40 mM | 0.0780 mL | 0.3901 mL | 0.7802 mL | 1.9504 mL | |
| 50 mM | 0.0624 mL | 0.3121 mL | 0.6241 mL | 1.5603 mL | |
| 60 mM | 0.0520 mL | 0.2601 mL | 0.5201 mL | 1.3003 mL | |
| 80 mM | 0.0390 mL | 0.1950 mL | 0.3901 mL | 0.9752 mL | |
| 100 mM | 0.0312 mL | 0.1560 mL | 0.3121 mL | 0.7802 mL |
S3969 Related Classifications
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