SML3971
A1899
≥97% (HPLC)
Synonym(s):
A 1899, A-1899, N-[(2,4-Difluorophenyl)methyl]-2′-[[[2-(4-methoxyphenyl)acetyl]amino]methyl][1,1′-biphenyl]-2-carboxamide, S 20951, S-20951, S20951
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About This Item
Empirical Formula (Hill Notation):
C30H26F2N2O3
CAS Number:
Molecular Weight:
500.54
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Pricing and availability is not currently available.
Quality Level
assay
≥97% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
Potent and selective TASK-1 potassium channel blocker that 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-1, KCNK3, IC50 = 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/kg, i.v.). Also mitigates the endothelin-1 induced prolonged action potential duration in cardiomyocytes (at 200 nM).
A1899 is a highly potent and selective non-voltage-dependent two-pore domain potassium channel K 2P 3.1 blocker (TASK-1, KCNK3, IC50 = 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/kg, i.v.). Also mitigates the endothelin-1 induced prolonged action potential duration in cardiomyocytes (at 200 nM).
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Identification of the A293 (AVE1231) Binding Site in the Cardiac Two-Pore-Domain Potassium Channel TASK-1: a Common Low Affinity Antiarrhythmic Drug Binding Site.
Cellular Physiology and Biochemistry, 52(5), 1223-1235 (2019)
Peadar B O'Donohoe et al.
Physiological reports, 6(19), e13876-e13876 (2018-10-05)
Sensing of hypoxia and acidosis in arterial chemoreceptors is thought to be mediated through the inhibition of TASK and possibly other (e.g., BKCa ) potassium channels which leads to membrane depolarization, voltage-gated Ca-entry, and neurosecretion. Here, we investigate the effects
A specific two-pore domain potassium channel blocker defines the structure of the TASK-1 open pore.
The Journal of Biological Chemistry, 286(16), 13977-13984 (2011)
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML3971-25MG | 04065271064072 |
| SML3971-5MG | 04065271064089 |