| Identification | Back Directory | [Name]
Kalydeco benzenesulfonate | [CAS]
1134822-09-5 | [Synonyms]
VX770 benzenesulfonate
VX-770 benzenesulfonate
VX 770 benzenesulfonate
Kalydeco benzenesulfonate
Ivacaftor (benzenesulfonate)
Ivacaftor benzenesulfonate (VX770)
Ivacaftor benzenesulfonate
(VX-770 benzenesulfonate
N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide.besylate | [Molecular Formula]
C30H34N2O6S | [MDL Number]
MFCD26960946 | [MOL File]
1134822-09-5.mol | [Molecular Weight]
550.67 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
≥55.1 mg/mL in DMSO; insoluble in H2O; ≥13.86 mg/mL in EtOH with gentle warming | [form ]
solid |
| Hazard Information | Back Directory | [Uses]
Ivacaftor Benzenesulfonate is a salt of Ivacaftor, a novel agent for the treatment of cystic fibrosis. | [Biological Activity]
ivacaftor (vx-770) is a cftr potentiator approved for patients with the g551d mutation of cystic fibrosis, which accounts for 4-5% cases of cystic fibrosis. | [in vitro]
in recombinant cells vx-770 increased cftr channel open probability (p(o)) in both the f508del processing mutation and the g551d gating mutation. vx-770 also increased cl(-) secretion in cultured human cf bronchial epithelia (hbe) carrying the g551d gating mutation on one allele and the f508del processing mutation on the other allele by approximately 10-fold, to approximately 50% of that observed in hbe isolated from individuals without cf [1]. | [in vivo]
at day 28, in the group of subjects who received 150 mg of vx-770, the median change in the nasal potential difference (in response to the administration of a chloride-free isoproterenol solution) from baseline was -3.5 mv (range, -8.3 to 0.5; p=0.02 for the within-subject comparison, p=0.13 vs. placebo), and the median change in the level of sweat chloride was -59.5 mmol per liter (range, -66.0 to -19.0; p=0.008 within-subject, p=0.02 vs. placebo) [2]. | [IC 50]
25 nm (f508del-cftr);100 nm (g551d-cftr) [1] |
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BOC Sciences
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Musechem
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InvivoChem
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