1134822-09-5 Usage
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]
Check Digit Verification of cas no
The CAS Registry Mumber 1134822-09-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,3,4,8,2 and 2 respectively; the second part has 2 digits, 0 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1134822-09:
(9*1)+(8*1)+(7*3)+(6*4)+(5*8)+(4*2)+(3*2)+(2*0)+(1*9)=125
125 % 10 = 5
So 1134822-09-5 is a valid CAS Registry Number.
1134822-09-5Relevant articles and documents
SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXAMIDE
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Page/Page column 49; 50; 51; 52, (2009/04/25)
Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.
