| Identification | Back Directory | [Name]
N-[(2,4-difluorophenyl)methyl]-2'-{[2-(4-methoxyphenyl)acetamido]methyl}-[1,1'-biphenyl]-2-carboxamide | [CAS]
498577-46-1 | [Synonyms]
A 1899
S20951
S-20951
S 20951
N-[(2,4-difluorophenyl)methyl]-2'-{[2-(4-methoxyphenyl)acetamido]methyl}-[1,1'-biphenyl]-2-carboxamide
[1,1'-Biphenyl]-2-carboxamide, N-[(2,4-difluorophenyl)methyl]-2'-[[[2-(4-methoxyphenyl)acetyl]amino]methyl]- | [Molecular Formula]
C30H26F2N2O3 | [MDL Number]
MFCD06407754 | [MOL File]
498577-46-1.mol | [Molecular Weight]
500.54 |
| Chemical Properties | Back Directory | [Boiling point ]
756.5±60.0 °C(Predicted) | [density ]
1.238±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
powder | [pka]
13.51±0.46(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [Biological Activity]
Potent and selective TASK-1 potassium channel blocker th at induces lasting respiratory alkalosis and stimulates breathing in anesthetized rats.
A1899 is a highly potent and selective non-voltage-dependent two-pore domain potassium channel K 2P 3.1 blocker (TASK-1KCNK3IC50 = 7 nM in CHO cells) with 10-fold selectivity over TASK-3 and much reduced or little potency towards TASK-2/4 (>8 μM in Xenopus oocytes) and other potassium channels. A1899 specifically blocks TASK-1 currents by 74% in Xenopus oocytes at 100 nM via an open-channel block mechanism. A1899 induces lasting respiratory alkalosis and stimulates breathing in anesthetized rats in vivo (5-25 mg/kgi.v.). Also mitigates the endothelin-1 induced prolonged action potential duration in cardiomyocytes ( at 200 nM). | [IC 50]
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) | [storage]
Store at -20°C | [References]
[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. DOI:10.1074/jbc.M111.227884
[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. DOI:10.1007/s00210-002-0599-x |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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