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此商品 | SAB3700848 | SAB3700576 | SAB3700539 |
|---|---|---|---|
| conjugate unconjugated | conjugate unconjugated | conjugate unconjugated | conjugate unconjugated |
| biological source rabbit | biological source goat | biological source rabbit | biological source goat |
| technique(s) immunohistochemistry: suitable, western blot: suitable, indirect ELISA: suitable | technique(s) ELISA: suitable, immunohistochemistry: suitable, western blot: suitable | technique(s) immunohistochemistry: suitable, indirect ELISA: suitable, western blot: suitable | technique(s) indirect ELISA: suitable, western blot: suitable |
| species reactivity rat | species reactivity rabbit | species reactivity rat | species reactivity rat |
| shipped in wet ice | shipped in wet ice | shipped in wet ice | shipped in wet ice |
生化/生理作用
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).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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)
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
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