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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.72%
- No. CAS: 498577-46-1
- Fòrmula: C30H26F2N2O3
- Peso molecular:500.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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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] |
Chemical Information
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No. CAS 498577-46-1
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Appearance Solid
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Peso molecular 500.54
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Fòrmula 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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Synonyms
S20951
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[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 Related Classifications
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