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Ivacaftor (VX-770)
| Product Name | Ivacaftor (VX-770) |
| Price: | Inquiry |
| Catalog No.: | CN00512 |
| CAS No.: | 873054-44-5 |
| Molecular Formula: | C24H28N2O3 |
| Molecular Weight: | 392.49 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=C(c1c[nH]c2c(c1=O)cccc2)Nc1cc(O)c(cc1C(C)(C)C)C(C)(C)C |
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| Description | Ivacaftor is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively. |
| Target | EC50: 100 nM (G551D-CFTR), 25 nM (F508del-CFTR)[1] |
| In Vitro | Ivacaftor (10 µM) increases 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) significantly increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells[2]. Ivacaftor shows no significant activity against 160 targets tested including the GABAA benzodiazepine receptor. Ivacaftor increases the chloride secretion with an EC50 of 0.236 ± 0.200 μM, a 10-fold shift in potency compared to the F508del HBEs[3]. In recombinant cells, VX-770 increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation. 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 | Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat[3]. |
| Density | 1.2±0.1 g/cm3 |
| Boiling Point | 550.5±50.0 °C at 760 mmHg |
| Flash Point | 286.7±30.1 °C |
| Exact Mass | 392.209991 |
| PSA | 85.68000 |
| LogP | 6.34 |
| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
| Storage condition | 2~8℃ |