Ivacaftor-d4
Based on 1 Customer Validation
Ivacaftor-d4 (VX-770-d4) is the deuterium labeled-Ivacaftor (HY-13017). Ivacaftor is a potent and orally active CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
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- Pureté: 97.32%
- Formule: C24H24D4N2O3
- Masse moléculaire:396.52
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Ivacaftor (10 μM) increases the PC secretion activity by 3-fold for ABCB4-G535D, 13.7-fold for ABCB4-G536R, 6.7-fold for ABCB4-S1076C, 9.4-fold for ABCB4-S1176L, and 5.7-fold for ABCB4-G1178S. Ivacaftor corrects the functional defect of ABCB4 mutants[1].
Ivacaftor (10 μM) significantly increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells[2].
Ivacaftor shows no significant activity against 160 targets tested including the GABAA benzodiazepine receptor. Ivacaftor increases the chloride secretion with an EC50 value of 0.236 ± 0.200 μM, a 10-fold shift in potency compared to the F508del HBEs[3].
In recombinant cells, Ivacaftor increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation. Ivacaftor increases forskolin-stimulated IT in temperature-corrected F508del-FRT cells by appr 6-fold with an EC50 of 25 nM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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Unlabeled Cas 873054-44-5
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Appearance Solid
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Masse moléculaire 396.52
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Formule C24H24D4N2O3
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Color White to off-white
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SMILES
O=C(C1=CNC2=C(C1=O)C([2H])=C([2H])C([2H])=C2[2H])NC3=CC(O)=C(C(C)(C)C)C=C3C(C)(C)C
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Synonyms
VX-770-d4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 50 mg/mL (126.10 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureté et documentation
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Fiche technique (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Delaunay JL, et al. Functional defect of variants in the adenosine triphosphate-binding sites of ABCB4 and their rescue by the cystic fibrosis transmembrane conductance regulator potentiator, ivacaftor (VX-770). Hepatology. 2017 Feb;65(2):560-570 [Content Brief]
[2]. Mutyam V, et al. Therapeutic benefit observed with the CFTR potentiator, ivacaftor, in a CF patient homozygous for the W1282X CFTR nonsense mutation. J Cyst Fibros. 2017 Jan;16(1):24-29 [Content Brief]
[3]. Hadida S, et al. Discovery of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, ivacaftor), a potent and orally bioavailable CFTR potentiator. J Med Chem. 2014 Dec 11;57(23):9776-9 [Content Brief]
[4]. Van Goor F, et al. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5219 mL | 12.6097 mL | 25.2194 mL | 63.0485 mL |
| 5 mM | 0.5044 mL | 2.5219 mL | 5.0439 mL | 12.6097 mL | |
| 10 mM | 0.2522 mL | 1.2610 mL | 2.5219 mL | 6.3049 mL | |
| 15 mM | 0.1681 mL | 0.8406 mL | 1.6813 mL | 4.2032 mL | |
| 20 mM | 0.1261 mL | 0.6305 mL | 1.2610 mL | 3.1524 mL | |
| 25 mM | 0.1009 mL | 0.5044 mL | 1.0088 mL | 2.5219 mL | |
| 30 mM | 0.0841 mL | 0.4203 mL | 0.8406 mL | 2.1016 mL | |
| 40 mM | 0.0630 mL | 0.3152 mL | 0.6305 mL | 1.5762 mL | |
| 50 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2610 mL | |
| 60 mM | 0.0420 mL | 0.2102 mL | 0.4203 mL | 1.0508 mL | |
| 80 mM | 0.0315 mL | 0.1576 mL | 0.3152 mL | 0.7881 mL | |
| 100 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL |
Ivacaftor-d4 Related Classifications
HY-13017S3 Related Classifications
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