Lumacaftor (VX-809)
- Product Name
- Lumacaftor (VX-809)
- CAS No.
- 936727-05-8
- Chemical Name
- Lumacaftor (VX-809)
- Synonyms
- Lumacaftor;VX-809;Lumacaftor(vx-809,vx809);3-[6-[[[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl]amino]-3-methyl-2-pyridinyl]benzoic acid;3-(6-{[1-(2,2-Difluoro-benzo[1,3]dioxol-5-yl)-cyclopropanecarbonyl]-amino}-3-methyl-pyridin-2-yl)-benzoicacid;CS-719;VRT 826809;3-(6-{[1-(2;VX809;VX-809;VX 809, >=98%
- CBNumber
- CB32489655
- Molecular Formula
- C24H18F2N2O5
- Formula Weight
- 452.41
- MOL File
- 936727-05-8.mol
Lumacaftor (VX-809) Property
- Melting point:
- 200-205oC
- Boiling point:
- 653.0±55.0 °C(Predicted)
- Density
- 1.51
- storage temp.
- -20°C Freezer
- solubility
- DMSO (Slightly), Methanol (Slightly)
- pka
- 3.95±0.10(Predicted)
- form
- Solid
- color
- White to Off-White
- InChI
- InChI=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)
- InChIKey
- UFSKUSARDNFIRC-UHFFFAOYSA-N
- SMILES
- C(O)(=O)C1=CC=CC(C2=NC(NC(C3(C4=CC=C5OC(F)(F)OC5=C4)CC3)=O)=CC=C2C)=C1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 22196
- Product name
- VX-809
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 22196
- Product name
- VX-809
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $151
- Updated
- 2024/03/01
- Product number
- 22196
- Product name
- VX-809
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $266
- Updated
- 2024/03/01
- Product number
- 22196
- Product name
- VX-809
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $573
- Updated
- 2024/03/01
- Product number
- 273822
- Product name
- VX-809
- Packaging
- 50mg
- Price
- $389
- Updated
- 2021/12/16
Lumacaftor (VX-809) Chemical Properties,Usage,Production
Uses
VX 809 is used in the stabilization of the CFTR protein used in the treatment of cystic fibrosis.
Definition
ChEBI: An aromatic amide obtained by formal condensation of the carboxy group of 1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropane-1-carboxylic acid with the aromatic amino group of 3-(6-amino-3-methylpyridin-2-yl)benzoic acid. Used for the treatment of cystic fi rosis.
Biological Activity
vx-809 is a cftr corrector that partially restores the function of f508del-cftr. in fischer rat thyroid (frt) cells, it increases f508del-cftr maturation at ec50 of 0.1 μm, and elevates f508del-cftr–mediated chloride transport at ec50 of 0.5 μm [1]. it has no effect of other ion channels (herg), transporter (p-gp) and disease-causing mislocalized proteins (α1-antitrypsin z mutant) [1]. vx-809 stabilizes n-terminal fragment of cftr that contain msd1 by altering its protein conformation [2, 3].homozygous f508del-cftr is the most common mutation in cystic fibrosis (cf) patients, accounting for 66–70% of cf cases worldwide. in cultured human bronchial epithelial cells that are homozygous for f508del, vx-809 restored the cftr function and improved chloride and fluid transport [1]. the combination of cftr potentiators and vx-809 further improved the function of f508del-cftr [4].vx-809 has been tested in several
target
CFTR
Mode of action
CF is a hereditary condition caused by mutations in the CFTR gene, which provides instructions for producing an ion channel protein called CF transmembrane conductance regulator (CFTR). These mutations cause defects in the CFTR protein, which disrupts the normal salt-water transport across the cell membrane and produces thick, sticky mucus that may accumulate in different organs, including the lungs. One of the common mutations in the CFTR gene is the so-called F508del mutation, which results in a defective misfolded CFTR protein. The misfolded protein is degraded by the cell before it can reach the cell membrane. Even if some of the defective proteins reach the cell membrane, they are unable to open correctly and allow the passage of chloride ions. Lumacaftor and ivacaftor work together to restore the function of the CFTR protein at the cell membrane. Lumacaftor increases the stability of defective CFTR proteins, helping them reach the cell membrane and stay there longer. But because it does not address the problem with the opening of the channel, lumacaftor is generally used in combination with ivacaftor, which acts on the defective proteins, helping them to open more often so that the salt-water balance across the cell surface is restored.
Lumacaftor (VX-809) Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Lumacaftor (VX-809) manufacturers
- Product
- Lumacaftor (VX-809) 936727-05-8
- Price
- US $0.00/g/Bag
- Min. Order
- 1g
- Purity
- 98.0%~102.0%
- Supply Ability
- 10kg/month
- Release date
- 2021-06-03
- Product
- Lumacaftor 936727-05-8
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-09-12
- Product
- Lumacaftor (VX-809) 936727-05-8
- Price
- US $0.00/KG
- Min. Order
- 0.1KG
- Purity
- 98%
- Supply Ability
- 1000KGS
- Release date
- 2023-07-14