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VX-809(Lumacaftor) Catalog No : 92219

Chemical Information

Product NameVX-809(Lumacaftor)
Iupac Chemical Name3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid 
SynonymsVX809; VX 809 
Molecular FormulaC24H18F2N2O5 
Molecular Weight452.41 
SmileO=C(O)C1=CC=CC(C2=NC(NC(C3(C4=CC=C(OC(F)(F)O5)C5=C4)CC3)=O)=CC=C2C)=C1
InChiKeyUFSKUSARDNFIRC-UHFFFAOYSA-N
InChiInChI=1S/C24H18F2N2O5/c1-13-5-8-19(27-20(13)14-3-2-4-15(11-14)21(29)30)28-22(31)23(9-10-23)16-6-7-17-18(12-16)33-24(25,26)32-17/h2-8,11-12H,9-10H2,1H3,(H,29,30)(H,27,28,31)
Cas936727-05-8

Technical Data

AppearanceSolid powder 
Purity98% 
SolubilitySoluble in DMSO 
Storage-20 ºC for 3 years 
Shipping ConditionShipped under ambient temperature 
Quality control

Description

From Wikipedia, the free encyclopedia

Lumacaftor (USAN, codenamed VX-809) is an experimental drug for the treatment of cystic fibrosis being developed by Vertex Pharmaceuticals. The drug is designed to be effective in patients that have the F508del mutation in the cystic fibrosis transmembrane conductance regulator (CFTR), the defective protein that causes the disease. F508del, meaning that the amino acid phenylalanine in position 508 is missing, is found in about 60% of cystic fibrosis patients in Europe, and in about 90% of persons with some mutation in the CFTR gene.

Lumacaftor acts on F508 CFTR during protein folding and suppresses misfolding.

Results from a Phase II clinical trial indicate that patients with the most common form of genetic mutation causing cystic fibrosishomozygous F508delhad a mean increase of 7.4% in lung function (FEV1) on a combination of lumacaftor and ivacaftor.However these results did not show a significant improvement in lung function.

 

Chemical Structure

92219 - VX-809(Lumacaftor) | CAS 936727-05-8

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