Tezacaftor-d4
Based on 1 Customer Validation
Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface.
For research use only. We do not sell to patients.
- Purity: 98.95%
- CAS No.: 1961280-24-9
- Formula: C26H23D4F3N2O6
- Molecular Weight:524.52
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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[1].
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[3][4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
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. 1961280-24-9
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Unlabeled Cas 1152311-62-0
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Appearance Solid
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Molecular Weight 524.52
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Formula C26H23D4F3N2O6
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Color White to off-white
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SMILES
FC1=C(C=C2C(N(C(C(C)(C)CO)=C2)C[C@@H](O)CO)=C1)NC(C3(C4=CC=C(OC(F)(O5)F)C5=C4)C([2H])([2H])C3([2H])[2H])=O
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Synonyms
VX-661-d4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (95.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9065 mL | 9.5325 mL | 19.0650 mL | 47.6626 mL |
| 5 mM | 0.3813 mL | 1.9065 mL | 3.8130 mL | 9.5325 mL | |
| 10 mM | 0.1907 mL | 0.9533 mL | 1.9065 mL | 4.7663 mL | |
| 15 mM | 0.1271 mL | 0.6355 mL | 1.2710 mL | 3.1775 mL | |
| 20 mM | 0.0953 mL | 0.4766 mL | 0.9533 mL | 2.3831 mL | |
| 25 mM | 0.0763 mL | 0.3813 mL | 0.7626 mL | 1.9065 mL | |
| 30 mM | 0.0636 mL | 0.3178 mL | 0.6355 mL | 1.5888 mL | |
| 40 mM | 0.0477 mL | 0.2383 mL | 0.4766 mL | 1.1916 mL | |
| 50 mM | 0.0381 mL | 0.1907 mL | 0.3813 mL | 0.9533 mL | |
| 60 mM | 0.0318 mL | 0.1589 mL | 0.3178 mL | 0.7944 mL | |
| 80 mM | 0.0238 mL | 0.1192 mL | 0.2383 mL | 0.5958 mL |
Tezacaftor-d4 Related Classifications
HY-15448S Related Classifications
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