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23

抑制剂 & 化合物

4

天然产物

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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 ...

化合物

Flecainide hydrochloride
Cat.No: T8581
Synonym:
Target: Others
NS3623
Cat.No: T16347
Synonym:
Target: Potassium Channel
NS5806
Cat.No: T16348
Synonym: NS-5806
Target: Potassium Channel
Flindokalner
Cat.No: T15286
Synonym: BMS-204352
Target: Potassium Channel
Clarithromycin
Cat.No: T1434
Synonym: A-56268,克拉霉素
Target: P450, ribosome, MRP, Antibacterial, Antibiotic, Autophagy
A2764 dihydrochloride
Cat.No: T7775
Synonym:
Target: Potassium Channel
ICA-105574
Cat.No: T9009
Synonym: ICA,3-nitro-N-[4-phenoxyphenyl]-benzamide
Target: HER
Sematilide hydrochloride
Cat.No: T3574
Synonym: 司美利特,CK-1752A,CK-1752,Sematilide HCl
Target: Potassium Channel
Linopirdine
Cat.No: T15758
Synonym: 利诺吡啶,DuP 996
Target: Potassium Channel, TRP/TRPV Channel
Ibutilide Fumarate
Cat.No: T6541
Synonym: Corvert Fumarate,U70226E,富马酸伊布利特
Target: Calcium Channel, Sodium Channel
DPO-1
Cat.No: T22745
Synonym:
Target: Potassium Channel
AM-92016 hydrochloride
Cat.No: T5585
Synonym:
Target: Potassium Channel
Azimilide Dihydrochloride
Cat.No: T7505
Synonym: NE-10064 Dihydrochloride,盐酸阿齐利特
Target: Potassium Channel
DPI 201-106
Cat.No: T27205
Synonym: DPI-201-106
Target: Sodium Channel
Dofetilide
Cat.No: T6476
Synonym: UK 68789,UK-68798,Tikosyn,多非利特
Target: Potassium Channel
AM92016
Cat.No: T70194
Synonym:
Target:
S9947
Cat.No: T69428
Synonym:
Target:
Zacopride
Cat.No: T5336L
Synonym: Racemic zacopride
Target:
Almokalant
Cat.No: T14189
Synonym: H 234​/09
Target: Potassium Channel
Ibutilide
Cat.No: T61685
Synonym:
Target:
Halofantrine hydrochloride
Cat.No: T15460
Synonym: WR-171669,SKF-102886
Target: Others
Tityustoxin-Kα
Cat.No: T80980
Synonym: TsTx-Kα
Target:
17R(18S)-EpETE
Cat.No: T36215
Synonym:
Target:
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.

天然产物

Ifenprodil Tartrate
Cat.No: T1186
Synonym:
Target: Potassium Channel, NMDAR, iGluR
Dronedarone
Cat.No: T7056
Synonym: 决奈达隆,SR 33589
Target: P450, Potassium Channel, Calcium Channel, Sodium Channel, Adrenergic Receptor, AChR, Autophagy
Resibufogenin
Cat.No: T4A2458
Synonym: 酯蟾毒配基,Bufogenin,Recibufogenin,酯蟾毒配基,蟾力苏
Target: Others
Chlorahololide C
Cat.No: TN3636
Synonym:
Target: Potassium Channel
TargetMol Loading
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