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AP14145 hydrochloride

CAS No. : 2387505-59-9

MCE 站：AP14145 hydrochloride

产品活性：AP14145 hydrochloride 是一种有效的 K_Ca2 (SK) 通道负变构调节剂，对 K_Ca2.2 (SK2) 和 K_Ca2.3 (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。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: AP14145 (10 nM-30 μM) inhibits both hK_Ca2.2 and hK_Ca2.3 channel currents in a concentration‐dependent fashion. AP14145 (10 μM) inhibits 50% of the hK_Ca1.1 current, 90% of the hK_Ca2.1 current and has no effect on hK_Ca3.1 channel. AP14145 (10 μM) increases the EC₅₀ of Ca²⁺ on K_Ca2.3 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 ?M. AP14145 inhibits hERG (K_V11.1) with an IC₅₀ of 71.8 ?M and K_ir3.1/K_ir3.4 (I_KACh) with an IC₅₀ of 9.3 ?M and does not produce any significant effects on K_V1.5 (I_Kur), K_V7.1/KCNE1 (I_Ks), K_V4.3/KChiP2 (I_to), and K_ir2.1 (I_K1) in 30 ?M or on Na_V1.5 (15 ?M; I_Na) on a panel of cardiac ion channels. AP14145 (1-10 ?M) produces no significant block of Ca_V1.2.

In Vivo: AP14145 (10 μM) increases the duration of the atrial effective refractory period (AERP) in isolated perfused rat hearts.
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).
AP14145 (5 mg/kg; bolus injections) has a C_max of 8355 nmol/L, a t_? of 24.3 minutes in landrace pigs (12-13 weeks old, 30-35 kg gilts).

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