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AP14145 hydrochloride

MCE 国际站：AP14145 hydrochloride

品牌：MedChemExpress (MCE)

货号：HY-120355A

CAS 号：2387505-59-9

生物活性：盐酸AP14145是一种强效的KCa2 (SK)通道负变构调节剂，对KCa2.2 (SK2)和KCa2.3 (SK3)通道的IC50值为1.1 µM。盐酸AP14145的抑制作用强烈依赖于通道中的两个氨基酸，即S508和A533。盐酸AP14145可延长大鼠的心房有效不应期(AERP)，并在对维纳卡兰耐药的猪房颤(AF)模型中表现出抗心律失常作用[1][2]。

体外研究(In Vitro)：AP14145 (10 nM-30 µM) inhibits both hKCa2.2 and hKCa2.3 channel currents in a concentration-dependent fashion. AP14145 (10 µM) inhibits 50% of the hKCa1.1 current, 90% of the hKCa2.1 current and has no effect on hKCa3.1 channel. AP14145 (10 µM) increases the EC50 of Ca2+ on KCa2.3 channels from 0.36 to 1.2 µM[1]. AP14145 hydrochloride demonstrates an IC50 in whole-cell patch clamp on the human SK3 channel of 1.3 µM. AP14145 inhibits hERG (KV11.1) with an IC50 of 71.8 µM and Kir3.1/Kir3.4 (IKACh) with an IC50 of 9.3 µM and does not produce any significant effects on KV1.5 (IKur), KV7.1/KCNE1 (IKs), KV4.3/KChiP2 (Ito), and Kir2.1 (IK1) in 30 µM or on NaV1.5 (15 µM; INa) on a panel of cardiac ion channels. AP14145 (1-10 µM) produces no significant block of CaV1.2[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：AP14145 (10 µM) increases the duration of the atrial effective refractory period (AERP) in isolated perfused rat hearts[1]. AP14145 (2.5 and 5 mg/kg; bolus injections (iv)) increases the duration of the atrial effective refractory period in male sprague-dawley rats (250-350 g, 1-3 months old)[1]. AP14145 (5 mg/kg; bolus injections) has a Cmax of 8355 nmol/L, a t of 24.3 minutes in landrace pigs (12-13 weeks old, 30-35 kg gilts)[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：398.81

Formula：C18H18ClF3N4O

性状：固体

颜色：White to off-white

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式： -20°C，密封保存，避免受潮 *溶剂保存：-80°C，6个月；-20°C，1个月（密封保存，避免受潮）

提供质量检测报告：Data Sheet、SDS、COA、元素分析报告、产品使用指南

产品活性：AP14145 hydrochloride 是一种有效的 KCa2 (SK) 通道负变构调节剂，对 KCa2.2 (SK2) 和 KCa2.3 (SK3) 通道的 IC50 均为 1.1 µM。AP14145 hydrochloride 的抑制作用很大程度上取决于通道中的两个氨基酸 S508 和 A533。AP14145 hydrochloride 延长了大鼠的心房有效不应期 (AERP)，并在耐 Vernakalant 的房颤 (AF) 猪模型中显示了抗心律失常作用。

IC50 & Target：IC50: 1.1 µM (KCa2.2) and 1.1 µM (KCa2.3)[1]

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参考文献：
[1]. Rafel Simó-Vicens, et al. A New Negative Allosteric Modulator, AP14145, for the Study of Small Conductance Calcium-Activated Potassium (KCa2) Channels. Br J Pharmacol. 2017 Dec;174(23):4396-4408.
[2]. Jonas Goldin Diness, et al. Termination of Vernakalant-Resistant Atrial Fibrillation by Inhibition of Small-Conductance Ca2+-Activated K + Channels in Pigs. Circ Arrhythm Electrophysiol. 2017 Oct;10(10):e005125.