Tezacaftor-d6
Tezacaftor-d6 (VX-661-d6) is deuterium labeled Tezacaftor. Tezacaftor (VX-661) is a F508del CFTR corrector. It helps CFTR protein reach the cell surface. However, Ivacaftor (VX-770, HY-13017), a CFTR potentiator, helps to prolong the opening time of cell surface CFTR protein channels. Tezacaftor combining with Ivacaftor, shows potent efficacy against cystic fibrosis and diseases with homozygous for the CFTR Phe508del mutation. Moreover, Elexacaftor (VX-445, HY-111772) is also a CFTR corrector. Elexacaftor-Tezacaftor-Ivacaftor aims at with cystic fibrosis (CF) with at least one Phe508del mutation, often avoids the indication for lung transplantation.
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- CAS No.: 1961280-94-3
- Formule: C26H21D6F3N2O6
- Masse moléculaire:526.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1961280-94-3
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Unlabeled Cas 1152311-62-0
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Masse moléculaire 526.53
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Formule C26H21D6F3N2O6
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SMILES
FC1=C(NC(C2(CC2)C3=CC=C4OC(OC4=C3)(F)F)=O)C=C5C(N(C[C@H](CO)O)C(C(C([2H])([2H])[2H])(CO)C([2H])([2H])[2H])=C5)=C1
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Synonyms
VX-661-d6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[3]. Taylor-Cousar JL, et al. Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del. N Engl J Med. 2017 Nov 23;377(21):2013-2023. [Content Brief]
[4]. Burgel PR, et al. Rapid Improvement after Starting Elexacaftor-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and Advanced Pulmonary Disease. Am J Respir Crit Care Med. 2021 Jul 1;204(1):64-73. [Content Brief]
[5]. Huang Y, et al. Elexacaftor/Tezacaftor/Ivacaftor Improved Clinical Outcomes in a Patient with N1303K-CFTR Based on In Vitro Experimental Evidence. Am J Respir Crit Care Med. 2021 Nov 15;204(10):1231-1235. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)