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21

抑制剂 & 化合物

2

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。
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。
TP1858L	Phe-Met-Arg-Phe, amide acetate Phe-Met-Arg-Phe, amide acetate（64190-70-1 freebase)	Potassium Channel	Membrane transporter/Ion channel
	Phe-Met-Arg-Phe, amide acetate(64190-70-1 freebase) 剂量依赖性 (ED50=23 nM) 激活肽能尾背神经元中的 K+ 电流。这种肽似乎在大脑的某些区域与神经肽 Y 一起定位。
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。
T31488	Dimethindene Dimetindeno,Z 2001,Dimetindene,二甲茚定,Z-2001,Z2001	Potassium Channel; Endogenous Metabolite; AChR; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
	Dimethindene (Dimetindeno) 是 H1受体的选择性拮抗剂，阻断 K+电流。Dimethindene 表现出抗组胺和抗胆碱作用。
T0723	Cloperastine hydrochloride HT-11 hydrochloride,盐酸氯哌斯丁	Potassium Channel; 5-HT Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Cloperastine hydrochloride (HT-11 hydrochloride) 是 hERG K+电流的抑制剂，IC50为 27 nM，具有浓度依赖性。
T0866	Propafenone Rythmol,普罗帕酮,Propafenonum	Potassium Channel; MRP; Sodium Channel	Immunology/Inflammation; Membrane transporter/Ion channel
	Propafenone (Propafenonum) 是钠通道阻滞剂，它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ，具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡，从而抑制食管癌增殖。
T13619	Cloperastine fendizoate Hustazol	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Cloperastine fendizoate (Hustazol) 是 hERG K+ 电流的抑制剂，IC50 为 27 nM。
T22662	Chromanol 293B	Others	Others
	slow delayed rectifier K+ current (IKs) blocker
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.
TP1440	Phe-Met-Arg-Phe amide trifluoroacetate
	Phe-met-arg-phe amide trifluoroacetate is an activator of K+ current with an ED50 of 23nm on the fundus nerve.
TP1858	Phe-Met-Arg-Phe, amide
	Phe-Met-Arg-Phe, amide dose dependently (ED50=23 nM) activates a K+ current in the peptidergic caudodorsal neurons. This peptide appears to localize with neuropeptide Y in some regions of the brain.
TP2090	AmmTX3
	KV4 channel blocker. Blocks A-type K+ current (ISA) in mouse cerebellar granule neurons. The accessory dipeptidyl peptidase-like proteins (DPP) 6 and 10 are required for blockade.
T80036	AmmTX3 TFA	Potassium Channel	Membrane transporter/Ion channel
	AmmTX3 TFA为来源于蝎子Androctonus mauretanicus毒液的肽类毒素，特异性拮抗Kv4通道，有效抑制A型K+电流（Ki: 131 nM）。
T68499	F15845 HBr
	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 suc...
T61197	Irdabisant hydrochloride
	Irdabisant (CEP-26401) hydrochloride 是一种选择性、口服活性的组胺H3受体拮抗剂/逆激动剂，具备良好的血脑屏障渗透性。该化合物对大鼠和人类的H3受体具有高亲和力，其Ki值分别为7.2 nM和2.0 nM。此外，Irdabisant hydrochloride在抑制hERG电流方面表现出较低的活性，IC50为13.8 μM。在大鼠社会认知模型中，它展现了认知增强和唤醒的效果，可作为精神分裂症或认知障碍研究的潜在工具。
T12879	Sematilide CK-1752	Others	Others
	Sematilide is a blocker of selective IKr channel.
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 ...
T2434	LY 303511	Potassium Channel; TNF; mTOR	Apoptosis; Membrane transporter/Ion channel; PI3K/Akt/mTOR signaling
	LY303511 是 LY294002 的结构类似物，可增强 SHEP-1 神经母细胞瘤细胞的TRAIL 敏感性，还可逆地阻断 MIN6 胰岛瘤细胞中的K+电流，IC50为64.6±9.1 μM。
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...

化合物

Flecainide hydrochloride

Cat.No: T8581

Target: Others

Ibutilide Fumarate

Cat.No: T6541

Synonym: Corvert Fumarate,U70226E,富马酸伊布利特

Target: Calcium Channel, Sodium Channel

Phe-Met-Arg-Phe, amide acetate

Cat.No: TP1858L

Synonym: Phe-Met-Arg-Phe, amide acetate（64190-70-1 freebase)

Target: Potassium Channel

Sematilide hydrochloride

Cat.No: T3574

Synonym: 司美利特,CK-1752A,CK-1752,Sematilide HCl

Target: Potassium Channel

Cat.No: T15758

Synonym: 利诺吡啶,DuP 996

Target: Potassium Channel, TRP/TRPV Channel

Cat.No: T31488

Synonym: Dimetindeno,Z 2001,Dimetindene,二甲茚定,Z-2001,Z2001

Target: Potassium Channel, Endogenous Metabolite, AChR, Histamine Receptor

Cloperastine hydrochloride

Cat.No: T0723

Synonym: HT-11 hydrochloride,盐酸氯哌斯丁

Target: Potassium Channel, 5-HT Receptor

Cat.No: T0866

Synonym: Rythmol,普罗帕酮,Propafenonum

Target: Potassium Channel, MRP, Sodium Channel

Cloperastine fendizoate

Cat.No: T13619

Synonym: Hustazol

Target: EGFR

Cat.No: T22662

Target: Others

Cat.No: T14189

Synonym: H 234/09

Target: Potassium Channel

Phe-Met-Arg-Phe amide trifluoroacetate

Cat.No: TP1440

Phe-Met-Arg-Phe, amide

Cat.No: TP1858

Cat.No: TP2090

Cat.No: T80036

Target: Potassium Channel

Cat.No: T68499

Irdabisant hydrochloride

Cat.No: T61197

Cat.No: T12879

Synonym: CK-1752

Target: Others

Cat.No: T36215

Cat.No: T2434

Target: Potassium Channel, TNF, mTOR

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Cat. No.	Product Name	Target	Signaling Pathways
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

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

Target: Potassium Channel

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