Emidurdar
Based on 6 publication(s) in Google Scholar
Endovion is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
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: 99.41%
- CAS 番号: 265646-85-3
- 分子式: C16H9BrF6N6O
- 分子量:495.18
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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Membrane Transporter/Ion Channel Compound Library
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MedChemExpress（MCE）の使用を引用している文献 Emidurdar
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生物活性
Endovion (NS3728, 10-100 μM) reduces TNFα-induced apoptosis and increases p53-protein level as well as downstream signaling, e.g., expression of p21Waf1/Cip1, Bax, Noxa, MDM2, and activation of Caspase-9/-3 in Cisplatin-sensitive cells[1].
Endovion (NS3728, 10 μM) inhibits cell proliferation in Capan-1, AsPC-1 and BxPC-3 cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Wild-type, resistant, and transiently transfected A2780 cells.
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Concentration:10-100 μM.
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Incubation Time:18 or 4.5 h.
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Result:Reduced the maximal taurine rate constant more than 90% compared with the untreated control cells.
Resulted in an increased LRRC8A protein expression.
Significantly reduceed p53 and p21Waf1/Cip1 protein level in A2780WT cells.
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Cell Line:Capan-1, AsPC-1, BxPC-3 and H6c7 cell lines.
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Concentration:10 μM.
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Incubation Time:24 h.
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Result:Resulted in the most pronounced inhibition in all cell lines with 77 ± 26 % in Capan-1, 67 ± 9 % in AsPC-1, and 54 ± 8 % in BxPC-3 cells at +67 mV.
化学情報
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CAS 番号 265646-85-3
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性状 Solid
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分子量 495.18
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分子式 C16H9BrF6N6O
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Color White to off-white
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SMILES
FC(F)(F)C1=CC(C(F)(F)F)=CC(NC(NC2=C(C3=NN=NN3)C=C(Br)C=C2)=O)=C1
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別名
Endovion; NS3728
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Nat Commun
2021 Jul 22;12(1):4457. PMID: 34294701 -
Virulence
LRRC8A promotes Glaesserella parasuis cytolethal distending toxin-induced p53-dependent apoptosis in NPTr cells. [Abstract]2023 Dec;14(1):2287339. PMID: 38018865 -
Int J Mol Sci
LRRC8A Inhibition Overcomes Chemoresistance by Downregulating MRP3 and CYP3A4 in the 3D Spheroid Model of Human Breast Cancer Cells. [Abstract]2026 Mar 13;27(6):2646. PMID: 41898509 -
Int J Mol Sci
Transcriptional Repression of CCL2 by KCa3.1 K+ Channel Activation and LRRC8A Anion Channel Inhibition in THP-1-Differentiated M2 Macrophages. [Abstract]2025 Aug 6;26(15):7624. PMID: 40806751 -
Int J Mol Sci
Downregulation of IL-8 and IL-10 by LRRC8A Inhibition through the NOX2-Nrf2-CEBPB Transcriptional Axis in THP-1-Derived M2 Macrophages. [Abstract]2024 Sep 5;25(17):9612. PMID: 39273558 -
Mol Oncol
2024 May 22. PMID: 38775167
溶剤 & 溶解度
DMSO : 125 mg/mL (252.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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 (277 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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取扱説明書 (2659 KB)
参考文献
[1]. Sørensen BH, et al. Downregulation of LRRC8A protects human ovarian and alveolar carcinoma cells against CDDP-induced expression of p53, MDM2, p21Waf1/Cip1, and Caspase-9/-3 activation. Am J Physiol Cell Physiol. 2016 Jun 1;310(11):C857-73. [Content Brief]
[2]. Sauter DR, et al. ANO1 (TMEM16A) in pancreatic ductal adenocarcinoma (PDAC). Pflugers Arch. 2015 Jul;467(7):1495-1508. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.0195 mL | 10.0973 mL | 20.1947 mL | 50.4867 mL |
| 5 mM | 0.4039 mL | 2.0195 mL | 4.0389 mL | 10.0973 mL | |
| 10 mM | 0.2019 mL | 1.0097 mL | 2.0195 mL | 5.0487 mL | |
| 15 mM | 0.1346 mL | 0.6732 mL | 1.3463 mL | 3.3658 mL | |
| 20 mM | 0.1010 mL | 0.5049 mL | 1.0097 mL | 2.5243 mL | |
| 25 mM | 0.0808 mL | 0.4039 mL | 0.8078 mL | 2.0195 mL | |
| 30 mM | 0.0673 mL | 0.3366 mL | 0.6732 mL | 1.6829 mL | |
| 40 mM | 0.0505 mL | 0.2524 mL | 0.5049 mL | 1.2622 mL | |
| 50 mM | 0.0404 mL | 0.2019 mL | 0.4039 mL | 1.0097 mL | |
| 60 mM | 0.0337 mL | 0.1683 mL | 0.3366 mL | 0.8414 mL | |
| 80 mM | 0.0252 mL | 0.1262 mL | 0.2524 mL | 0.6311 mL | |
| 100 mM | 0.0202 mL | 0.1010 mL | 0.2019 mL | 0.5049 mL |
Emidurdar 関連分類
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