CFTR activator 1
Based on 1 Customer Validation
CFTR activator 1 is a potent and selective CFTR activator, with an EC50 of 23 nM. CFTR activator 1 can be used to ameliorate dry eye disease.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 2768261-09-0
- Formula: C27H27N5O4
- Molecular Weight:485.53
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Membrane Receptor-targeted Compound Library
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Highly Selective Activators Library
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Bioactive Compound Library
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Biological Activity
EC50: 23 nM (CFTR)[1]
CFTR activator 1 (compound 16d) (30 nM-10 μM) potently activates CFTR chloride channel in FRT cells expressing human CFTR, with an EC50 of 342 nM in the presence of 50 nM Forskolin[1].
CFTR activator 1 (30 μM; pretreated for 10 min or 5 min) does not affect channel activities of ANO1 and VRAC in FRT cells expressing human ANO1 and in LN215 cells expressing a halide sensors YFP-F46L/H148Q/I152L[1].
CFTR activator 1 (30 μM; 10 min) slightly increases cAMP level compared to the control in CHO-K1 cells[1].
CFTR activator 1 (30 μM; 48 h) does not affect the cell viability of CorE and ConjE[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CFTR activator 1 (0.1 mg/eye; single topical instillation of eye drops) is well distributed in CFTR-expressing target tissues (cornea and conjunctiva) of male New Zealand White Rabbit, is maintained for a long period of time, and has a negligible systemic exposure[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight weeks old female C57BL/6J mice were injected Scopolamine hydrobromide[1]
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Dosage:2060 μM, 5 μL, and maintained for 30 s
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Administration:Eye drop application was done in both eyes, three times a day (11:00 am, 2:00 pm, 5:00 pm) for 10 days
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Result:Enhanced tear secretion and improved corneal erosion.
Reduced mRNA expression of pro-inflammatory cytokines including IL-1β, IL-17, and TNF-α and MMP2 in cornea and conjunctiva.
Chemical Information
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CAS No. 2768261-09-0
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Appearance Solid
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Molecular Weight 485.53
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Formula C27H27N5O4
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Color White to light yellow
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SMILES
O=C(N1C[C@@H](N(CC1)C(C2=CC=CC=C2)=O)C)C3=NN4C(C5=CC(OC)=C(C=C5)OC)=CC=NC4=C3
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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
DMSO : 100 mg/mL (205.96 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)
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 (5.15 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 (5.15 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.
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 (280 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0596 mL | 10.2980 mL | 20.5960 mL | 51.4901 mL |
| 5 mM | 0.4119 mL | 2.0596 mL | 4.1192 mL | 10.2980 mL | |
| 10 mM | 0.2060 mL | 1.0298 mL | 2.0596 mL | 5.1490 mL | |
| 15 mM | 0.1373 mL | 0.6865 mL | 1.3731 mL | 3.4327 mL | |
| 20 mM | 0.1030 mL | 0.5149 mL | 1.0298 mL | 2.5745 mL | |
| 25 mM | 0.0824 mL | 0.4119 mL | 0.8238 mL | 2.0596 mL | |
| 30 mM | 0.0687 mL | 0.3433 mL | 0.6865 mL | 1.7163 mL | |
| 40 mM | 0.0515 mL | 0.2575 mL | 0.5149 mL | 1.2873 mL | |
| 50 mM | 0.0412 mL | 0.2060 mL | 0.4119 mL | 1.0298 mL | |
| 60 mM | 0.0343 mL | 0.1716 mL | 0.3433 mL | 0.8582 mL | |
| 80 mM | 0.0257 mL | 0.1287 mL | 0.2575 mL | 0.6436 mL | |
| 100 mM | 0.0206 mL | 0.1030 mL | 0.2060 mL | 0.5149 mL |
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