A1899
Based on 1 Customer Validation
A1899 is a potent and highly selective blocker of the K2P channel TASK-1. A1899 has IC50 values of 35.1 nM and 7 nM for TASK-1 channels expressed in oocytes and CHO cells, respectively. A1899 is also an IKur blocker that can be used for the research of cardiovascular 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: 99.72%
- CAS 番号: 498577-46-1
- 分子式: C30H26F2N2O3
- 分子量:500.54
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保管条件:Powder -20°C, 3 years , 4°C, 2 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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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
生物活性
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TASK-1 0.035 μM (IC50) |
TASK-3 0.318 pg/mL (IC50) |
TASK-2 12 μM (IC50) |
TASK-4 8.1 μM (IC50) |
TREK-1 23.8 μM (pIC50) |
TREK-2 8.4 μM (IC50) |
TRAAK >20 μM (IC50) |
THIK-1 2.2 μM (IC50) |
TRESK 0.9 μM (IC50) |
Kv1.1 2.7 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.007 μM
Compound: 1; A1899
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Inhibition of human TASK1 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay
Inhibition of human TASK1 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay
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[PMID: 31260312] |
| CHO | IC50 |
0.07 μM
Compound: 1; A1899
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Inhibition of human TASK3 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay
Inhibition of human TASK3 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay
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[PMID: 31260312] |
| CHO | IC50 |
12 μM
Compound: 1; A1899
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Inhibition of human TASK2 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay
Inhibition of human TASK2 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay
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[PMID: 31260312] |
| CHO | IC50 |
7 nM
Compound: 1, A-1899
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Inhibition of TASK-1 (unknown origin) expressed in CHO cells by thallium flux assay
Inhibition of TASK-1 (unknown origin) expressed in CHO cells by thallium flux assay
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[PMID: 25017033] |
| CHO | IC50 |
8.1 μM
Compound: 1; A1899
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Inhibition of human TASK4 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay
Inhibition of human TASK4 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay
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[PMID: 31260312] |
| Oocyte | IC50 |
1.2 μM
Compound: 17m
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Inhibition of human voltage-gated potassium channel subunit Kv1.5 expressed in Xenopus oocytes
Inhibition of human voltage-gated potassium channel subunit Kv1.5 expressed in Xenopus oocytes
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[PMID: 12570371] |
化学情報
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CAS 番号 498577-46-1
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性状 Solid
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分子量 500.54
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分子式 C30H26F2N2O3
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Color Off-white to light yellow
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SMILES
O=C(NCC1=CC=C(C=C1F)F)C2=CC=CC=C2C3=CC=CC=C3CNC(CC4=CC=C(C=C4)OC)=O
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別名
S20951
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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 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (249.73 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 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]. Streit AK, et al. A specific two-pore domain potassium channel blocker defines the structure of the TASK-1 open pore. J Biol Chem. 2011 Apr 22;286(16):13977-84. [Content Brief]
[2]. Knobloch K, et al. Electrophysiological and antiarrhythmic effects of the novel I(Kur) channel blockers, S9947 and S20951, on left vs. right pig atrium in vivo in comparison with the I(Kr) blockers dofetilide, azimilide, d,l-sotalol and ibutilide. Naunyn Schmiedebergs Arch Pharmacol. 2002 Nov;366(5):482-7. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9978 mL | 9.9892 mL | 19.9784 mL | 49.9461 mL |
| 5 mM | 0.3996 mL | 1.9978 mL | 3.9957 mL | 9.9892 mL | |
| 10 mM | 0.1998 mL | 0.9989 mL | 1.9978 mL | 4.9946 mL | |
| 15 mM | 0.1332 mL | 0.6659 mL | 1.3319 mL | 3.3297 mL | |
| 20 mM | 0.0999 mL | 0.4995 mL | 0.9989 mL | 2.4973 mL | |
| 25 mM | 0.0799 mL | 0.3996 mL | 0.7991 mL | 1.9978 mL | |
| 30 mM | 0.0666 mL | 0.3330 mL | 0.6659 mL | 1.6649 mL | |
| 40 mM | 0.0499 mL | 0.2497 mL | 0.4995 mL | 1.2487 mL | |
| 50 mM | 0.0400 mL | 0.1998 mL | 0.3996 mL | 0.9989 mL | |
| 60 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8324 mL | |
| 80 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6243 mL | |
| 100 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4995 mL |
A1899 関連分類
HY-103067 関連分類
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