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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8581 |
Flecainide hydrochloride
|
Others | Others |
Flecainide hydrochloride 是一种用于预防和治疗异常快速心率的药物。这包括室性和室上性心动过速。 | |||
T16347 |
NS3623
|
Potassium Channel | Membrane transporter/Ion channel |
NS3623 是 hERG1 (KV11.1)钾通道激活剂,激活IKr 和Ito 电流,具有抗心律失常作用。NS3623也是 hERG1 通道抑制剂。 | |||
T16348 |
NS5806
NS-5806 |
Potassium Channel | Membrane transporter/Ion channel |
NS5806 是钾电流的激活剂,可增加 KV4.3/KChIP2峰值电流幅度,EC50值为 5.3 μM。它会在包含 KChIP2 的通道复合体中降低 KV4.2 和 KV4.3 电流衰减。 | |||
T15286 |
Flindokalner
BMS-204352 |
Potassium Channel | Membrane transporter/Ion channel |
Flindokalner (BMS-204352) 是一种钾离子通道调节剂。它是大电导钙激活 K 通道正向调节剂。它是在 HEK293 细胞中表达的所有神经元 Kv7通道亚型的正调节剂。它在 Kv7.1 通道 (Ki=3.7 μM) 处显示负调节活性,并充当 GABAA 受体的负调节剂。它在体内显示出抗焦虑功效。 | |||
T1434 |
Clarithromycin
A-56268,克拉霉素 |
P450; ribosome; MRP; Antibacterial; Antibiotic; Autophagy | Autophagy; Immunology/Inflammation; Metabolism; Microbiology/Virology |
Clarithromycin (A-56268) 具有广谱的抗菌活性。它抑制 CYP3A4催化的三唑仑 α-羟基化,IC50(Ki) 值为 56 (43) μM。它抑制 HERG 钾电流。它可削弱连接 hERG1 和 PI3K 的信号通路影响自噬流 。 | |||
T7775 |
A2764 dihydrochloride
|
Potassium Channel | Membrane transporter/Ion channel |
A2764 dihydrochloride 是高选择性的TRESK (K2P18.1)抑制剂,对 TREK-1 和 TALK-1 有抑制作用。它相比基底 mTRESK 电流,对激活渠道更敏感 (IC50= 6.8 μM)。它可导致细胞去极化,增加细胞的兴奋性,在探索 TRESK 通道在偏头痛和痛觉中的作用中具有研究的价值。 | |||
T9009 |
ICA-105574
ICA,3-nitro-N-[4-phenoxyphenyl]-benzamide |
HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
ICA-105574 (ICA) 是 hERG 通道激活剂。它通过消除 hERG 通道的失活从而增强 hERG 通道活性。它可以把电流幅度急剧增加到原来的 10 倍以上,其EC50值为 0.5 +/- 0.1 μM,Hill 斜率 (n(H)) 为 3.3 +/- 0.2。 | |||
T3574 |
Sematilide hydrochloride
司美利特,CK-1752A,CK-1752,Sematilide HCl |
Potassium Channel | Membrane transporter/Ion channel |
Sematilide hydrochloride (CK-1752) 是一种选择性的 IKr 通道阻滞剂。Sematilide 以浓度依赖性抑制延迟整流钾通道 (K+current),IC50为 25 μM。Sematilide 是一种 III 类抗心律不齐剂。 | |||
T15758 |
Linopirdine
利诺吡啶,DuP 996 |
Potassium Channel; TRP/TRPV Channel | Membrane transporter/Ion channel |
Linopirdine (DuP 996) 是一种口服有效的,选择性 M 型 K+电流 (IM;Kv7;KCNQ Channels) 抑制剂,IC50为 2.4 μM。Linopirdine 是TRPV1激活剂。Linopirdine 是一种公认的认知增强药物,可增加大鼠脑组织中乙酰胆碱的释放。 | |||
T6541 |
Ibutilide Fumarate
Corvert Fumarate,U70226E,富马酸伊布利特 |
Calcium Channel; Sodium Channel | Membrane transporter/Ion channel; Metabolism |
Ibutilide Fumarate (U70226E) 是一种 III 类抗心律失常药物,可作用于急性心梗阻塞。 | |||
T22745 |
DPO-1
|
Potassium Channel | Membrane transporter/Ion channel |
DPO-1 可以高效抑制电压门控钾离子通道Kv1.5,也可以阻断超快速延迟整流钾电流。它能够预防房性心律失常。 | |||
T5585 |
AM-92016 hydrochloride
|
Potassium Channel | Membrane transporter/Ion channel |
AM-92016 hydrochloride 是一种整流钾电流的特异性阻断剂。它能够延迟整流钾通道,使膜复极化,限制神经冲动的持续时间。 | |||
T7505 |
Azimilide Dihydrochloride
NE-10064 Dihydrochloride,盐酸阿齐利特 |
Potassium Channel | Membrane transporter/Ion channel |
Azimilide Dihydrochloride (NE-10064 Dihydrochloride) 是 I(Ks) 和 I(Kr) 抑制剂,具有抗心律失常活性。 | |||
T27205 |
DPI 201-106
DPI-201-106 |
Sodium Channel | Membrane transporter/Ion channel |
DPI 201-106对电压门控钠通道的有心脏选择性调节活性,从而产生正性肌力作用。DPI 201-106 具有协同肌膜和细胞内作用机制。 | |||
T6476 |
Dofetilide
UK 68789,UK-68798,Tikosyn,多非利特 |
Potassium Channel | Membrane transporter/Ion channel |
Dofetilide (UK 68789) 是一种具有口服活性、有效的且特异性的IKr 阻滞剂,作为 III 类抗心律失常药物。Dofetilide 可用于心血管疾病研究。 | |||
T70194 |
AM92016
|
||
AM92016 is a specific blocker of the time dependent delayed rectifier potassium current. AM92016 does not show any β-adrenoceptor blocking activity. | |||
T69428 |
S9947
|
||
S9947 is a Kv1.5/IKur channel blocker, suppressing both cloned (Kv1.5) and native (IKur) cardiac potassium current. | |||
T5336L |
Zacopride
Racemic zacopride |
||
Zacopride is a selective agonist of inward rectifier potassium current (I K1) channel, inhibiting ventricular arrhythmias without affecting atrial arrhythmias. | |||
T14189 |
Almokalant
H 234/09 |
Potassium Channel | Membrane transporter/Ion channel |
Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker. And it inhibits a specific component (Ikr) of the time-dependent delayed rectifier K+ current. | |||
T61685 |
Ibutilide
|
||
Ibutilide (U70226E free base) is a potent antiarrhythmic compound that extends the action potential duration. It effectively blocks the rapidly activating delayed rectifier potassium current (I Kr ) in AT-1 cells [1]. | |||
T15460 |
Halofantrine hydrochloride
WR-171669,SKF-102886 |
Others | Others |
Halofantrine hydrochloride is a blocker of delayed rectifier potassium current. Halofantrine hydrochloride also via the inhibition of the human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial agent. | |||
T80980 |
Tityustoxin-Kα
TsTx-Kα |
||
Tityustoxin-Kα (TsTx-Kα) 为钾电压门控通道抑制剂,表现出对培养的海马神经元持续外向电流的剂量依赖性阻断作用。 | |||
T36215 |
17R(18S)-EpETE
|
||
17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases ... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1186 |
Ifenprodil Tartrate
|
Potassium Channel; NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
Ifenprodil tartrate 是典型的非竞争性 NMDA 受体拮抗剂,抑制 GIRK (Kir3),通过基底 GIRK 活性减少内向电流,有用做脑血管舒张试剂的潜力。它对 NR1A/NR2B 受体亲和力是 NR1A/NR2A 受体的 400 倍。 | |||
T7056 |
Dronedarone
决奈达隆,SR 33589 |
P450; Potassium Channel; Calcium Channel; Sodium Channel; Adrenergic Receptor; AChR; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Dronedarone (SR 33589) 是一种胺碘酮类似物,对治疗心房颤动可能有效。它是CYP3A4的底物和中度抑制剂。它是多种离子电流的有效阻滞剂,通过非竞争性结合到肾上腺素能受体显示出抗肾上腺素能的效果。 | |||
T4A2458 |
Resibufogenin
酯蟾毒配基,Bufogenin,Recibufogenin,酯蟾毒配基,蟾力苏 |
Others | Others |
Resibufogenin (Bufogenin) 是华蟾素的成分之一,表现出抑制氧化应激及肿瘤再生的活性。 | |||
TN3636 | Chlorahololide C | Potassium Channel | Membrane transporter/Ion channel |
Chlorahololide C is a potent and selective potassium channel blocker, it exerts potent and selective inhibition on the delayed rectifier (I(K)) K(+) current with the IC(50) value of 3.6 +/- 10.1 mu M. |