Nesolicaftor
Based on 2 publication(s) in Google Scholar
Nesolicaftor (PTI-428) is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.37%
- No. CAS: 1953130-87-4
- Fòrmula: C18H18N4O4
- Peso molecular:354.36
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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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Publications Citing Use of MedChemExpress (MCE) Nesolicaftor
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Actividad biológica
CFTR[1]
Nesolicaftor (PTI-428) (30 μM, 24 h) can increase CFTR function, such as causing a larger change in inh-172 in 16HBE14o-cells expressing G542X-CFTR, also can increase in F508del-CFTR function of CFBE41o-cells expressing F508del-CFTR in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1953130-87-4
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Appearance Solid
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Peso molecular 354.36
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Fòrmula C18H18N4O4
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Color White to off-white
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SMILES
O=C(C1=CC(C2=CC=CC=C2)=NO1)N[C@H]3C[C@H](C4=NN=C([C@H](O)C)O4)C3
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Synonyms
PTI-428
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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 (2)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
The CFTR Amplifier Nesolicaftor Rescues TGF-β1 Inhibition of Modulator-Corrected F508del CFTR Function. [Abstract]2022 Sep 19;23(18):10956. PMID: 36142862 -
J Cyst Fibros
2021 May;20(3):452-459. PMID: 32674984
Solvente y solubilidad
DMSO : 250 mg/mL (705.50 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, 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: ≥ 2.08 mg/mL (5.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (5.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Mijnders M, et al. Correcting CFTR folding defects by small-molecule correctors to cure cystic fibrosis. Curr Opin Pharmacol. 2017 Jun;34:83-90. [Content Brief]
[2]. Arianna Venturini, et al. Comprehensive Analysis of Combinatorial Pharmacological Treatments to Correct Nonsense Mutations in the CFTR Gene. Int J Mol Sci. 2021 Nov 4;22(21):11972. [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, 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 | 2.8220 mL | 14.1099 mL | 28.2199 mL | 70.5497 mL |
| 5 mM | 0.5644 mL | 2.8220 mL | 5.6440 mL | 14.1099 mL | |
| 10 mM | 0.2822 mL | 1.4110 mL | 2.8220 mL | 7.0550 mL | |
| 15 mM | 0.1881 mL | 0.9407 mL | 1.8813 mL | 4.7033 mL | |
| 20 mM | 0.1411 mL | 0.7055 mL | 1.4110 mL | 3.5275 mL | |
| 25 mM | 0.1129 mL | 0.5644 mL | 1.1288 mL | 2.8220 mL | |
| 30 mM | 0.0941 mL | 0.4703 mL | 0.9407 mL | 2.3517 mL | |
| 40 mM | 0.0705 mL | 0.3527 mL | 0.7055 mL | 1.7637 mL | |
| 50 mM | 0.0564 mL | 0.2822 mL | 0.5644 mL | 1.4110 mL | |
| 60 mM | 0.0470 mL | 0.2352 mL | 0.4703 mL | 1.1758 mL | |
| 80 mM | 0.0353 mL | 0.1764 mL | 0.3527 mL | 0.8819 mL | |
| 100 mM | 0.0282 mL | 0.1411 mL | 0.2822 mL | 0.7055 mL |
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