1134822-09-5 Usage
Uses
Used in Pharmaceutical Industry:
Kalydeco benzenesulfonate is used as a therapeutic agent for the treatment of cystic fibrosis. It functions by targeting the defective CFTR protein, which is responsible for the disease's symptoms, and helps to improve its function. This results in the alleviation of the respiratory and digestive issues associated with cystic fibrosis, enhancing the quality of life for patients.
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 academic research and scientific papers
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.
