货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V47513-5mg	≥98%	￥6660.00 V47513-5mg ￥6660.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V47513-5mg

≥98%

￥6660.00

货期：3-5天

产品描述：

AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).

体外研究：

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.
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.

保存条件：

-20°C, 干燥

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.507 ml	12.537 ml	25.075 ml
5 mM	0.501 ml	2.507 ml	5.015 ml
10 mM	0.251 ml	1.254 ml	2.507 ml
50 mM	0.05 ml	0.251 ml	0.501 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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