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Tezacaftor

Product Name
Tezacaftor
CAS No.
1152311-62-0
Chemical Name
Tezacaftor
Synonyms
tezacaftor(VX661);(R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-Methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxaMide;VX-661;CS-956;Tezacaftor;VX-661/VX661;VX661/Tezacaftor;VX-661 USP/EP/BP;VX 661; VX661;VX-661;VX 661;VX661;VX-661; TEZACAFTOR
CBNumber
CB22632076
Molecular Formula
C26H27F3N2O6
Formula Weight
520.5
MOL File
1152311-62-0.mol
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Tezacaftor Property

Boiling point:
610.8±55.0 °C(Predicted)
Density 
1.49±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C , stored under nitrogen
solubility 
≥21.8 mg/mL in DMSO; insoluble in EtOH; ≥24.3 mg/mL in H2O
form 
solid
pka
13.99±0.20(Predicted)
color 
White to yellow
InChIKey
MJUVRTYWUMPBTR-MRXNPFEDSA-N
SMILES
C1(C2=CC=C3OC(F)(F)OC3=C2)(C(NC2C(F)=CC3=C(C=2)C=C(C(C)(C)CO)N3C[C@@H](O)CO)=O)CC1
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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.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21480
Product name
VX-661
Purity
≥98%
Packaging
5mg
Price
$62
Updated
2024/03/01
Cayman Chemical
Product number
21480
Product name
VX-661
Purity
≥98%
Packaging
10mg
Price
$115
Updated
2024/03/01
Cayman Chemical
Product number
21480
Product name
VX-661
Purity
≥98%
Packaging
25mg
Price
$239
Updated
2024/03/01
Cayman Chemical
Product number
21480
Product name
VX-661
Purity
≥98%
Packaging
50mg
Price
$448
Updated
2024/03/01
TRC
Product number
T321510
Product name
Tezacaftor
Packaging
1mg
Price
$55
Updated
2021/12/16
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Tezacaftor Chemical Properties,Usage,Production

Description

Tezacaftor (VX-661) is an oral medication for cystic fibrosis (CF) developed by Vertex Pharmaceuticals. In a combination therapy formulation called Symdeko (tezacaftor plus ivacaftor), it is approved in the U.S. and Canada for CF patients, ages 12 and older, who have two copies of the F508del mutation in the CFTR gene and one minimal function mutation. Symdeko is approved and marketed in the EU as Symkevi.Tezacaftor is not approved as a stand-alone treatment, but as part of a combination therapy.

Uses

Tezacaftor is used as a combination therapy with Ivacaftor for the treatment of patients with cystic fibrosis.

Indications

Tezacaftor is combined with ivacaftor in one product for the treatment of cystic fibrosis (CF) in patients aged 12 years or older with two copies of the F508del gene mutation or at least one mutation in the CFTR gene that is responsive to this drug.
Tezacaftor, when used in combination with ivacaftor and elexacaftor in the product Trikafta, is also indicated for the treatment of CF in patients 12 years of age and older that have at least one F508del mutation in the CFTR gene.

Definition

VX-661 is an investigational compound that promotes the maturation of delta F508 mutants of the cystic fibrosis transmembrane conductance regulator (CFTR). Delta F508 CFTR represents a class of CFTR mutation that is characterized by impaired processing of misfolded CFTR proteins and reduced accumulation of the protein at the cell surface. VX-661 is intended to facilitate trafficking of CFTR to the epithelial cell membrane. It may be combined with the CFTR potentiator ivacaftor (Item No. 15145) to stimulate both CFTR accumulation and opening at the apical epithelial surface.

Biochem/physiol Actions

VX-661 is another cystic fibrosis transmembrane conductance regulator (CFTR) corrector in development for the treatment of cystic fibrosis.

Mechanism of action

The transport of charged ions across cell membranes is normally achieved through the actions of the cystic fibrosis transmembrane regulator (CFTR) protein. This protein acts as a channel and allows for the passage of chloride and sodium. This process affects the movement of water in and out of the tissues. It impacts the production of mucus that lubricates and protects certain organs and body tissues, including the lungs. In the F508del mutation of the CFTR gene, one amino acid is deleted at position 508. Therefore, the CFTR channel function is compromised, resulting in thickened mucus secretions. CFTR correctors such as tezacaftor aim to repair F508del cellular misprocessing. This is done by modulating the position of the CFTR protein on the cell surface to the correct position, allowing for adequate ion channel formation and increased water and salt movement through the cell membrane. The concomitant use of ivacaftor is intended to maintain an open channel, increasing the transport of chloride and reducing thick mucus production.

in vitro

VX-661, is CFTR modulator that is potentially useful for treatment of cystic fibrosis. VX-661 corrects F508del-CFTR trafficking and increases F508del-CFTR protein activity in vitro.

target

F508 del CFTR

References

[1] s. donaldson, j. pilewski, m. griese, q. dong, p.-s. lee, for the vx11–661-101 study group. ws7.3 vx-661, an investigational cftr corrector, in combination with ivacaftor, a cftr potentiator, in patients with cf and homozygous for the f508del-cftr mutation: interim analysis. journal of cystic fibrosis, volume 12, supplement 1, june 2013, page s14

Tezacaftor Preparation Products And Raw materials

Raw materials

Preparation Products

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Tezacaftor Suppliers

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View Lastest Price from Tezacaftor manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Tezacaftor 1152311-62-0
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
100kg/Month
Release date
2024-10-09
Wuhan Nutra Biotechnology Co.,Ltd
Product
tezacaftor;VX661 1152311-62-0
Price
US $0.00-0.00/g
Min. Order
1g
Purity
98%
Supply Ability
1000kgs
Release date
2021-05-23
Qingdao RENAS Polymer Material Co., Ltd.
Product
VX-661 1152311-62-0
Price
US $0.00/kg
Min. Order
20kg
Purity
99%
Supply Ability
20 tons
Release date
2024-10-29

1152311-62-0, TezacaftorRelated Search:


  • VX 661;VX661;VX-661; TEZACAFTOR
  • VX-661
  • VX-661/VX661
  • 1-(2,2-Difluoro-1,3-benzodioxol-5-yl)-N-[1-[(2R)-2,3-dihydroxypropyl]-6-fluoro-2-(2-hydroxy-1,1-dimethylethyl)-1H-indol-5-yl]-cyclopropanecarboxamide
  • (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-Methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxaMide
  • Cyclopropanecarboxamide, 1-(2,2-difluoro-1,3-benzodioxol-5-yl)-N-[1-[(2R)-2,3-dihydroxypropyl]-6-fluoro-2-(2-hydroxy-1,1-dimethylethyl)-1H-indol-5-yl]-
  • 1-(2,2-Difluoro-1,3-benzodioxol-5-yl)-N-[1-[(2R)-2,3-dihydroxypropyl]-6-fluoro-2-(2-hydroxy-1,1-dimethylethyl)-1H-indol-5-yl]-cyclopropanecarboxamide VX661
  • 1-(2,2-difluoro-1,3-benzodioxol-5-yl)-N-[1-[(2R)-2,3-dihydroxypropyl]-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)indol-5-yl]cyclopropane-1-carboxamide
  • (R)-1-(2,2-Difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-
  • VX 661; VX661;VX-661
  • VX661/Tezacaftor
  • CS-956
  • tezacaftor(VX661)
  • VX-661 USP/EP/BP
  • Tezacaftor D4Q: What is Tezacaftor D4 Q: What is the CAS Number of Tezacaftor D4
  • inhibit,Tezacaftor,Inhibitor,VX-661,Cystic fibrosis transmembrane conductance regulator,Autophagy,VX 661,CFTR
  • N,3,3-Trimethyl-1,5-dioxaspiro[5.5]undecan-9-amine Hydrochloride (4-Methylaminocyclohexanone 2',2'-Dimethyltrimethylene Ketal Hydrochloride)
  • (R)-1-(2,2-Difluorobenzo[d][1,3]dioxol-5-yl)-N-[1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methyl-2-propyl)-5-indolyl]cyclopropanecarboxamide
  • Tezacaftor
  • 1152311-62-0
  • C26H27F3N2O6
  • Inhibitors
  • API