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Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 1-2 weeks | 1-2 weeks | |
| 50 mg | $1,980 | 1-2 weeks | 1-2 weeks | |
| 100 mg | $2,500 | 1-2 weeks | 1-2 weeks |
| Description | Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment. |
| In vitro | Ivacaftor displays no significant activity against 160 targets tested including the GABAA benzodiazepine receptor. Ivacaftor enhances the chloride secretion (EC50 of 0.236 ± 0.200 μM). Compared to the F508del HBEs, it has a 10-fold shift in potency [3]. Ivacaftor (10?μM) enhances the PC secretion activity by 3-fold for ABCB4-G535D, 13.7-fold for ABCB4-G536R, 6.7-fold for ABCB4-S1076C, 9.4-fold for ABCB4-S1176L, and 5.7-fold for ABCB4-G1178S. Ivacaftor corrects the functional defect of ABCB4 mutants[1]. Ivacaftor (10 μM) obviously increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells[2]. VX-770 increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation, in recombinant cells. VX-770 increases forskolin-stimulated IT in temperature-corrected F508del-FRT cells by appr 6-fold with an EC50 of 25 nM[4]. |
| In vivo | In rat, Ivacaftor (1-200 mg/kg, p.o.) shows good oral bioavailability[3]. |
| Synonyms | VX-770 hydrate |
| Molecular Weight | 410.514 |
| Formula | C24H30N2O4 |
| Cas No. | 1134822-07-3 |
| Smiles | O.CC(C)(C)c1cc(c(NC(=O)c2c[nH]c3ccccc3c2=O)cc1O)C(C)(C)C |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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