Conditionnement : 5mg
Synonyms: VX-445
| Description | Elexacaftor (VX-445) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It promotes the processing and trafficking of CFTR, increases the amount of CFTR on the cell surface, and improves the processing and trafficking of Phe508del CFTR protein. |
| Targets & IC50 | CFTR:1.01 μM |
| In vitro | Elexacaftor (VX-445) has the potential to treat cystic fibrosis and it also is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore Phe508del CFTR protein function. VX-445-Tezacaftor-VX-770 significantly improves Phe508del CFTR protein processing, trafficking, chloride transport. To a greater extent than any two of these agents in dual combination[2]. |
| In vivo | METHODS: Patients with the Phe508del–Phe508del genotype underwent a 4-week run-in of tezacaftor and ivacaftor and were randomized to receive either elexacaftor (VX-445) (200 mg orally daily) plus tezacaftor (100 mg daily) and ivacaftor (150 mg daily) or matching placebo plus tezacaftor and ivacaftor for 4 weeks. RESULTS Treatment with elexacaftor (VX-445)-tezacaftor-ivacaftor significantly increased the percentage predicted FEV1 by up to 13.8 percentage points in patients with the Phe508del-MF genotype and up to 11.0 percentage points in patients with the Phe508del-Phe508del genotype who were already receiving tezacaftor-ivacaftor.[2] |
| Synonyms | VX-445 |
| Molecular Weight | 597.65 |
| Formula | C26H34F3N7O4S |
| Cas No. | 2216712-66-0 |
| Smiles | C(NS(=O)(=O)C1=CN(C)N=C1C)(=O)C2=C(N=C(C=C2)N3N=C(OCC(C(F)(F)F)(C)C)C=C3)N4C[C@@H](C)CC4(C)C |
| Relative Density. | 1.38 g/cm3 (Predicted) |
| Storage | Store at low temperature,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 125 mg/mL (209.15 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (6.69 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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