nav1.5

AZD 7009是一种新型抗心律失常化合物，对CHO K1细胞中 hNav1.5的钠电流具有抑制作用，IC50为11 uM。AZD 7009 对离体兔心房和心室肌细胞的晚期钠电流具有抑制作用，对e -4031诱导的动作电位持续时间延长具有抑制作用，促使浦肯野纤维的早期后去极化(EADs)。

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

Sulcardine 2HCl 是一种多离子通道阻滞剂，具有抗心律失常作用，可阻断 hERG 和hNav1.5通道的特性，可用于研究心房颤动和室性心律失常。

GNE-0439 是一种新型Nav1.7 选择性抑制剂，IC50为0.34 μM，同时可抑制 Nav1.5（IC50=38.3 μM）及突变型N1742K通道（IC50=0.37 μM）。其羧酸基团结合于通道孔外区域，与已知的 VSD4 选择性配体机制不同，因此是离子通道研究中的重要化合物。

GFB-8438 是有效的TRPC5选择性抑制剂，对 hTRPC5 和 hTRPC4 的IC50分别为 0.18 和 0.29 μM。它对 TRPC6、其他 TRP 家族成员、NaV1.5 具有良好的选择性，对 hERG 通道的活性也有限。它对小鼠足细胞的保护作用。

Nav1.1 activator 1(compound 4)是一种有效的和血脑屏障通透性的Nav1.1激动剂，对 Nav1.2、Nav1.5、Nav1.6 有显著的选择性，能够在0.03 μM电流下增加Nav 1.1的衰减时间常数，可用于研究中枢神经系统疾病。

AZD7507 是口服具有活力的CSF-1R 抑制剂，具有抗肿瘤作用。

DPP8/9-IN-2 (Compound 21) 是一种有效的DPP8/9抑制剂，IC50分别为0.22 nM和3 nM，Ki分别为2.9 nM和6 nM。此化合物具有一定的心脏毒性，对hERG钾通道、Nav1.5钠通道以及Cav1.2钙通道的IC50分别为0.7 μM、29.0 μM和27.7 μM。DPP8/9-IN-2 可用于研究肿瘤等相关疾病。

Norquetiapine (N-Desalkylquetiapine) 是 Quetiapine 的代谢产物，作为选择性 HCN1 通道抑制剂，其 IC50 为 13.9 μM。它选择性地抑制去甲肾上腺素的再摄取，是 5-HT1A 受体的部分激动剂 (Ki = 45 nM)，并且表现为前突触 α2 (Ki = 237 nM)、5-HT2C (Ki = 107 nM) 和 5-HT7 (Ki = 76 nM) 受体的拮抗剂。Norquetiapine 还能以状态依赖的方式阻断人体心脏钠通道 Nav1.5，且在 LPS 注射的 C57BL/6 小鼠中显示出一定的抗炎效果。该化合物可用于抑郁症和炎症的研究。

TC-N 1752 是一种具有口服活性的 Nav1.7 通道抑制剂，IC50 为 0.17 μM。 TC-N 1752 显示镇痛活性。

GS-462808 is a late sodium current inhibitor of the cardiac Nav1.5 channel. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

4,9-Anhydrotetrodotoxin (4,9-anhydro-TTX) is a derivative of TTX that selectively blocks inward sodium current through Nav1.6 voltage-activated sodium channels (IC50 = 7.8 nM in Xenopus oocytes). [1][2][3] It demonstrates IC50 values of 1.3, 0.34, 0.99, 78.5, 1.3, and >30 µM for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1]

GDC-0310是一种选择性和可口服的Nav1.7抑制剂，对人Nav1.7的IC50=0.6 nM，可用于研究疼痛。

VGSC blocker-1 is a powerful small molecule that serves as a blocker for the neonatal isoform of the VGSC subtype known as Nav1.5 (nNav1.5). It effectively blocks INa peak currents by 34.9% at a concentration of 1 μM, and demonstrates a 0.3% inhibition of cell invasion at the same concentration in the MDA-MB-231 human breast cancer cell line, without compromising cell viability.

F 15845 is a blocker of the persistent sodium current prevents consequences of hypoxia in rat femoral artery. F15845 has been shown to selectively inhibit the persistent sodium current of Nav1.5[1] exerting cardioprotective effects following ischemia. In vitro testing showed minimal effects of F15845 on other important ion channels of the heart, including major Ca2+ and K+ channels.[1] This characteristic is thought to account for the limited effect of F15845 to change other heart parameters such as basal cardiac function, hemodynamic functions and ventricular fibrillation. F15845 was also shown to exert improved effects when the membrane potential was depolarized,[1] by acting on the extracellular side of the channel.

AA43279 is a novel selective Nav1.1 activator, increasing the firing activity of parvalbumin-expressing, fast-spiking GABAergic interneurons and increasing the spontaneous inhibitory post-synaptic currents (sIPSCs) recorded from pyramidal neurons.

Flecainide acetate (R-818) 是位于心脏的 Nav1.5钠离子通道的阻断剂，具有抗心律失常的作用。

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) 是强效的、广谱的电压门控钠通道阻滞剂，对人 Nav1.1 和 Nav1.3 亚型具有等效选择性，IC50分别为 13 nM 和 23 nM。它对Nav1.2 的抑制作用较弱，IC50为240 nM，对 Nav1.4、Nav1.6、抗TTX 的人 Nav1.5、Nav1.8 通道表现出大于 1000 倍的选择性，IC50>10 μM。

Phrixotoxin 3 TFA 是一种高效的电压门控钠通道阻滞剂，对NaV1.2、NaV1.3、NaV1.4、NaV1.1及NaV1.5的IC50值分别为0.6、42、72、288和610 nM。该化合物通过改变门控动力学的去极化并阻断钠电流的内向流，调控电压门控钠通道，表现出类似典型门控修饰毒素的作用机制。

Phlo1b（μ-TrTx-Phlo1b）为含35个氨基酸残基的肽毒素，特异性抑制Nav1.7通道。相较之下，其对Nav1.2与Nav1.5的抑制作用较弱。

Phlo1a（μ-TrTx-Phlo1a）是含35个氨基酸残基的肽类毒素。Phlo1b为选择性Nav1.7抑制剂，而Phlo1a对Nav1.2与Nav1.5显示较低的抑制活性。

Ceratotoxin-1 (CcoTx1)为电压门控钠通道亚型的抑制剂，特别是对Nav1.1/β1、Nav1.2/β1、Nav1.4/β1和Nav1.5/β1具有不同程度的抑制效果，其IC50值分别为523 nM、3 nM、888 nM和323 nM。此外，Ceratotoxin-1对Nav1.8/β1亦有抑制作用。

Jingzhaotoxin XI (JZTX-XI) 为抑制钠电导的化合物，其IC50值为124 nM。该化合物能够减缓CHO-K1细胞中Nav1.5通道的快速失活，EC50值为1.18±0.2 μM。