N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide
N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide
CAS: 873054-44-5
Molecular Formula: C24H28N2O3
N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide - Names and Identifiers
| Name | N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide |
| Synonyms | VX-770 Ivacaftor VX 770, Ivacaftor Ivacaftor (VX-770) N-(2,4-Di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxaMide N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide 3-QuinolinecarboxaMide, N-[2,4-bis(1,1-diMethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo- N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide Ivacaftor (VX-770) |
| CAS | 873054-44-5 |
| InChI | InChI=1/C24H28N2O3/c1-23(2,3)16-11-17(24(4,5)6)20(27)12-19(16)26-22(29)15-13-25-18-10-8-7-9-14(18)21(15)28/h7-13,27H,1-6H3,(H,25,28)(H,26,29) |
N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide - Physico-chemical Properties
| Molecular Formula | C24H28N2O3 |
| Molar Mass | 392.49 |
| Density | 1.187 |
| Melting Point | 212-215°C |
| Boling Point | 550.4±50.0 °C(Predicted) |
| Flash Point | 286.7°C |
| Solubility | DMSO (Slightly), Ethyl Acetate (Slightly), Methanol (Slightly) |
| Vapor Presure | 1E-12mmHg at 25°C |
| Appearance | Solid |
| Color | White to Light Brown |
| pKa | 11.08±0.23(Predicted) |
| Storage Condition | Refrigerator |
| Refractive Index | 1.605 |
| Use | Ivacaftor (VX-770) is an enhancer of cystic fibrosis transmembrane conduction regulator (CFTR), which targets G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM respectively. |
| In vitro study | Ivacaftor(10 μm) significantly increased forskolin-stimulated Cl in Fisher rat thyroid (FRT) cells expressing CFTR mutant G551D |
| In vivo study | Ivacaftor acts on cystic fibrosis subjects aged 6 to 11 carrying the G551D mutation and has completed Phase III study. |
N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide - Risk and Safety
| HS Code | 29333990 |
N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.548 ml | 12.739 ml | 25.478 ml |
| 5 mM | 0.51 ml | 2.548 ml | 5.096 ml |
| 10 mM | 0.255 ml | 1.274 ml | 2.548 ml |
| 5 mM | 0.051 ml | 0.255 ml | 0.51 ml |
Last Update：2024-01-02 23:10:35
N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide - Reference Information
| Introduction | Ivacato (trade name Kalydeco) is a drug used to treat human cystic fibrosis (CFTR) gene (mainly G551D mutation) that regulates specific gene mutations in cystic fibrosis transmembrane conduction, accounting for 4-5 cases of cystic fibrosis. It is also included in a combination of drugs, lumacaftor / ivacaftor (trade name orkambi), which is used to treat cystic fibrosis patients who have F508del mutations in CFTR. |
| mechanism of action | Ivacaftor is a synergist of CFTR protein. The CFTR protein is a chloride channel that exists on the surface of epithelial cells of multiple organs. Ivacaftor facilitates increased chloride transport through enhanced CFTR protein channel opening probability (or gating). |
| Indications | KALYDECO is a cystic fibrosis transmembrane conductance regulator (CFTR) synergist, suitable for the treatment of 6 months and above Patients with a mutation in the CFTR gene, based on clinical and/or in vitro assay data, the mutation responds to ivacaftor. |
| cystic fibrosis compound drug | on July 2, 2015, FDA approved the listing of Lumacato/ivacato (Lumacaftor Ivacaftor) compound tablets, a new drug for cystic fibrosis treated by Vertex biotechnology pharmaceutical company, with Orkambi trade names. Cystic fibrosis is an autosomal recessive genetic disease. Its cause is that the gene mutation of cystic fibrosis transmembrane conduction regulator causes a large amount of mucus to block the exocrine glands of the whole body. The clinical manifestations are chronic obstructive pulmonary disease, Pancreatic insufficiency and abnormal increase in sweat sodium and chlorine caused by sweat gland involvement. The disease is more common among white people in Europe and North America, and Forte Corporation of the United States is listed through priority approval channels. |
| biological activity | Ivacaftor (VX-770) is a selective enhancer of CFTR, which targets G551D-CFTR and F508del-CFTR. EC50 in fisher rat thyroid cells is 100 nM and 25 nM respectively. |
| target | TargetValue F508del-CFTR (Fisher rat thyroid cells) 25 nM(EC50) G551D-CFTR (Fisher rat thyroid cells) 100 nM(EC50) |
| Target | Value |
| F508del-CFTR (Fisher rat thyroid cells) | 25 nM(EC50) |
| G551D-CFTR (Fisher rat thyroid cells) | 100 nM(EC50) |
| in vitro study | Ivacaftor(10 μM) acts on Fisher rat thyroid (FRT) cells expressing CFTR mutant G551D, significantly increasing forskolin-stimulated Cl |
| in vivo study | Ivacaftor acts on cystic fibrosis subjects aged 6 to 11 carrying G551D mutation, and has completed phase III study. |
Last Update：2024-04-10 22:29:15
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Product Name: Ivacaftor (VX-770) Visit Supplier Webpage Request for quotation
CAS: 873054-44-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 873054-44-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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