Vanzacaftor
Based on 5 publication(s) in Google Scholar
Vanzacaftor (VX-121) is an orally active noval corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves processing and trafficking of CFTR protein as well as increases chloride transport in triple combined with Tezacaftor (HY-15448) and Deutivacaftor. Vanzacaftor-Tezacaftor-Deutivacaftor is safe and well tolerated, improving lung function, respiratory symptoms, and CFTR function with cystic fibrosis, which is promising for research in the field of cystic fibrosis diseases.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.72%
- CAS 番号: 2374124-49-7
- 分子式: C32H39N7O4S
- 分子量:617.76
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Vanzacaftor
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生物活性
Vanzacaftor (0-10 μM) stimulates K+ secretion at low micromolar concentrations in human bronchial epithelial cells (HBEs), which is inhibited by Paxilline (HY-N6778) with an EC50 of 4.4 μM [2]. Vanzacaftor (1 μM, 5 μM, 10 μM) significantly potentiates αBKCa current density, which is blocked by Paxilline (HY-N6778) in HEK cells[2]. Vanzacaftor (5 μM) reduces action potential firing frequency and alters neuronal excitability in a primary hippocampal neuron[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2374124-49-7
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性状 Solid
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分子量 617.76
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分子式 C32H39N7O4S
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Color Off-white to light yellow
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SMILES
CC(C)(C[C@@](CCC/N=C1NC(S(=O)(N2)=O)=CC=C\1)([H])C3)N3C4=NC(N(C=C5)N=C5OCCC6C7(CC7)C68CC8)=CC=C4C2=O
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別名
VX-121
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (5)
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Journal Impact Factor
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Most Recent
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J Cyst Fibros
Vanzacaftor-Tezacaftor as an alternative therapeutic resource for the ETI-Resistant L467F-F508del Allele: Ex vivo prediction and exploratory clinical assessment. [Abstract]2026 Jun 4:S1569-1993(26)01638-3. PMID: 42243036 -
Am J Physiol Cell Physiol
(R)-vanzacaftor potentiates BKCa channels in the absence of CFTR correction or potentiation. [Abstract]2025 Oct 1;329(4):C1130-C1138. PMID: 40920663 -
PNAS Nexus
VX-445 (elexacaftor) inhibits chloride secretion across human bronchial epithelial cells by directly blocking KCa3.1 channels. [Abstract]2025 Jul 4;4(7):pgaf211. PMID: 40688096 -
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溶剤 & 溶解度
DMSO : 100 mg/mL (161.88 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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (276 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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取扱説明書 (2659 KB)
参考文献
[1]. Uluer AZ, et al. Safety and efficacy of vanzacaftor-tezacaftor-deutivacaftor in adults with cystic fibrosis: randomised, double-blind, controlled, phase 2 trials[J]. Lancet Respir Med. 2023 Jun;11(6):550-562. [Content Brief]
[2]. Kolski-Andreaco A, et al. Potentiation of BKCa channels by cystic fibrosis transmembrane conductance regulator (CFTR) correctors VX-445 and VX-121[J]. J Clin Invest. 2024 Jul 2:e176328. [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 (stored under nitrogen). 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 | 1.6188 mL | 8.0938 mL | 16.1875 mL | 40.4688 mL |
| 5 mM | 0.3238 mL | 1.6188 mL | 3.2375 mL | 8.0938 mL | |
| 10 mM | 0.1619 mL | 0.8094 mL | 1.6188 mL | 4.0469 mL | |
| 15 mM | 0.1079 mL | 0.5396 mL | 1.0792 mL | 2.6979 mL | |
| 20 mM | 0.0809 mL | 0.4047 mL | 0.8094 mL | 2.0234 mL | |
| 25 mM | 0.0648 mL | 0.3238 mL | 0.6475 mL | 1.6188 mL | |
| 30 mM | 0.0540 mL | 0.2698 mL | 0.5396 mL | 1.3490 mL | |
| 40 mM | 0.0405 mL | 0.2023 mL | 0.4047 mL | 1.0117 mL | |
| 50 mM | 0.0324 mL | 0.1619 mL | 0.3238 mL | 0.8094 mL | |
| 60 mM | 0.0270 mL | 0.1349 mL | 0.2698 mL | 0.6745 mL | |
| 80 mM | 0.0202 mL | 0.1012 mL | 0.2023 mL | 0.5059 mL | |
| 100 mM | 0.0162 mL | 0.0809 mL | 0.1619 mL | 0.4047 mL |
Vanzacaftor 関連分類
HY-145603 関連分類
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