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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。 | |||
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。 | |||
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。 | |||
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。 | |||
T5336L |
Zacopride
Racemic zacopride |
Others | Others |
Zacopride is a selective agonist of inward rectifier potassium current (I K1) channel, inhibiting ventricular arrhythmias without affecting atrial arrhythmias. | |||
T70194 |
AM92016
|
Others | Others |
AM92016 is a specific blocker of the time dependent delayed rectifier potassium current. AM92016 does not show any β-adrenoceptor blocking activity. | |||
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. | |||
T69428 |
S9947
|
Others | Others |
S9947 is a Kv1.5/IKur channel blocker, suppressing both cloned (Kv1.5) and native (IKur) cardiac potassium current. | |||
T61685 |
Ibutilide
|
Others | Others |
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
|
Others | Others |
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. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01889 |
KCNK3 Protein, Human, Recombinant (His & Myc)
Potassium channel subfamily K member 3,TWIK-related... |
Human | E. coli |
pH-dependent, voltage-insensitive, background potassium channel protein. Rectification direction results from potassium ion concentration on either side of the membrane. Acts as an outward rectifier when external potassium concentration is low. When external potassium concentration is high, current is inward. KCNK3 Protein, Human, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 50.5 kDa and the accession number is O... |