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36

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T23101	o-3M3FBS	Others	Others
	o-3M3FBS 是 m-3M3FBS 的阴性对照。它以独立于 PLC 的机制及拮抗方式抑制内向和外向电流。它以与 m-3M3FBS 竞争的方式增加 [Ca2+]i 增加。
T22408	Proflavine 吡啶-3,6-二胺,3,6-Diaminoacridine	Antibacterial	Microbiology/Virology
	Proflavine (3,6-Diaminoacridine) 是吖啶染料，可用作抗菌剂。它是 DNA 嵌入剂，能够阻滞Kir3.2孔。它用作与 Kir3.2 相关的神经系统疾病的研究。
T0438	Proflavine Hemisulfate 3,6-Diaminoacridine hemisulfate,Proflavin hemisulfate,硫酸原黄素	Others; Potassium Channel; DNA; Thrombin; Antibacterial; Autophagy	Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Others; Proteases/Proteasome
	Proflavine Hemisulfate (3,6-Diaminoacridine hemisulfate) 是一种 DNA 嵌入剂，也是一种吖啶染料。它是抗菌剂，也可作为 Kir3.2孔阻滞剂，可研究与 Kir3.2 相关的神经系统疾病。
T4542	Clonixin Clonixic acid,氯尼辛	Others	Others
	Clonixin (Clonixic acid) 是一种非甾体抗炎药，具有口服活性。
T21263	Amlodipine maleate Amlodipine (+-)-form maleate,Amvaz	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Amlodipine maleate (Amvaz) 是一种具有口服活性的二氢吡啶类钙通道阻滞剂，通过阻滞电压依赖性 L 型钙通道，从而抑制钙离子内流。Amlodipine maleate 可用于研究高血压和癌症。
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。
T36033	DETA NONOate NOC-18,Diethylamine NONOate	NO Synthase	Immunology/Inflammation
	DETA NONOate (NOC 18)是外源性一氧化氮 (NO) 供体，具有血管舒张和抗抑郁活性。DETA NONOate 可用于激活神经元中的内向电流，可加速MRSA感染伤口的愈合。
T22361	Mepivacaine Carbocaine	Sodium Channel	Membrane transporter/Ion channel
	Mepivacaine (Carbocaine) 是一种可用于局部麻醉的酰胺类化合物，可使人或动物短暂的失去自知觉。Mepivacaine 通过与神经细胞膜上特定的电压门控钠离子通道结合，抑制钠离子内流和膜去极化来发挥作用。Mepivacaine 适用于神经阻滞和硬膜外麻醉。
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。
T0207	Ranolazine dihydrochloride 盐酸雷诺嗪,雷诺嗪二盐酸盐,RS 43285,Ranolazine 2HCl	Calcium Channel; Sodium Channel; Autophagy	Autophagy; Membrane transporter/Ion channel; Metabolism
	Ranolazine dihydrochloride (Ranolazine 2HCl) 是一种抗心绞痛和抗缺血剂，可通过抑制内向钠电流的后期作用来发挥功效，而不会影响心率或血压。它对 INa 和 IKr 的 IC50值分别为 6 μM 和 12 μM。它还是脂肪酸氧化的部分抑制剂。
T15555	IK1 inhibitor PA-6	Potassium Channel	Membrane transporter/Ion channel
	IK1 inhibitor PA-6 是一种喷他脒类似物，是选择性的 IK1(KIR2.x 离子通道携带向内整流电流) 抑制剂，对人和老鼠中 KIR2.x 电流的 IC50值为 12-15 nM。它可上调 KIR2.1 的蛋白表达，诱导细胞内 KIR2.1 的蛋白的积累。它在房颤和心律失常的研究中具有潜力。
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。
T13387L	Zatebradine hydrochloride UL-FS-49CL,UL-FS-49	Others; HCN Channel	Membrane transporter/Ion channel; Others
	Zatebradine hydrochloride (UL-FS-49CL) 是一种高效的、有效的HCN Channel 抑制剂( IC50 ：1.96 µM)。 HCN Channel 是一种有效的超极化激活环核苷酸门控通道。 Zatebradine hydrochloride 阻止通过人类 HCN1，HCN2，HCN3 和 HCN4 通道的缓慢内向电流，其 IC50 值分别为 1.83 µM，2.21 µM，1.90 µM 和 1.88 µM。
T2535	Ivabradine hydrochloride 盐酸伊伐布雷定,S 16257-2,Ivabradine HCl	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Ivabradine hydrochloride (S 16257-2) 是一种可口服的，超极化激活的环核苷酸门控离子通道通道阻滞剂。
T19839	Oxatomide Oxatomida	P2X Receptor; Calcium Channel; 5-HT Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
	Oxatomide (Oxatomida) 是一种有效且具有口服活性的双重 H1 组胺受体和 P2X7 受体双重拮抗剂，具有抗组胺和抗过敏活性。Oxatomide 可用于阻断人 P2X7 受体中 ATP 诱导的电流，IC50 为 0.95 μM。Oxatomide 对 ATP 诱导的 Ca2+ 内流具有抑制作用，IC50 值为 0.43 μM。Oxatomide 对 5-羟色胺具有抑制作用。Oxatomide可用于治疗免疫系统疾病和研究超敏反应。
T23012	MNI caged kainic acid	Others	Others
	Generates large inward currents at resting membrane potential
T24948	VU625 VU007625,VU 625,VU 007625,VU-625,VU-007625
	VU625 is an effective inhibitor of Aedes aegypti inward rectifier potassium channels.
T71406	SA 2572
	SA 2572 is a newly synthesized Ca2+ antagonist having a inhibitory effect on the fast Na+ inward channel.
T5336L	Zacopride Racemic zacopride
	Zacopride is a selective agonist of inward rectifier potassium current (I K1) channel, inhibiting ventricular arrhythmias without affecting atrial arrhythmias.
T68361	Asocainol hydrochloride
	Asocainol hydrochloride ia an antiarrhythmic drug which inhibits slow Ca2+ influx. This is accompanied by alterations in normal Na+-carried action potentials. Therefore, Asocainol not only inhibits Ca2+ inflow but also interferes with the fast inward Na+ current.
T80510	Tertiapin-RQ	Potassium Channel	Membrane transporter/Ion channel
	Tertiapin-RQ为抗抑郁特性的内向整流K+通道阻滞剂肽。
T70063	GYKI 52466 HCl
	GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of general...
TP1967	Phrixotoxin 3
	Potent blocker of voltage-gated sodium channels (IC50 values are 0.6, 42, and 72 nM for NaV1.2, NaV1.3 and NaV1.5 respectively). Blocks inward sodium currents in a voltage-dependent manner.
T17240	VU041	Others	Others
	VU041 is an inhibitor of Anopheles gambiae and Aedes aegypti inward rectifier potassium 1 channels (IC50: 2.5 μM and 1.7 μM, respectively). VU041 inhibits appreciably is mammalian Kir2.1 (IC50: 12.7 μM) and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1.
T37093	4,9-Anhydrotetrodotoxin 4,9-Anhydrotetrodotoxin,4,9-anhydro-TTX
	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 &#181M for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1]
TP2114	Tertiapin-Q
	A high affinity blocker for inward-rectifier K+ channels, this compound is a stable derivative of the bee venom toxin tertiapin. Binds to ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with high affinity (Ki values are 1.3 and 13.3 nM respectively) and
T36740	Guanosine 5’-diphosphate (sodium salt hydrate)
	Guanosine 5’-diphosphate (GDP) is a purine nucleotide and biosynthetic precursor of guanosine 5’-triphosphate .1It has been used to study the conformations of GTPases.2GDP (100 μM) activates sulfonylurea receptor 2B (SUR2B) linked to the inward-rectifier potassium channel 6.1 (Kir6.1) in HEK293T cells in a patch-clamp assay.3 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Biochemistry(2002) 2.Vetter, I.R., and Wittinghofer, A.The guanine nucleotide-binding switch in three dimensionsScience294(5545)...
T63445	Amlodipine mesylate
	Amlodipine mesylate 是口服具有活力的二氢吡啶钙通道（calcium channel）阻滞剂，能够阻断电压依赖性的 L 型钙通道，并抑制钙离子内流，是一种抗心绞痛药。Amlodipine mesylate 能够用于研究高血压和癌症。
T37199	Bilaid C
	Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the μ-opioid receptor (EC50= 4.2 μM). 1.Dekan, Z., Siana...
T70987	AT-1001
	AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal prepar...
T41209	DPNB-ABT 594
	DPNB-ABT 594 is a nitrobenzyl-caged ABT 594, a selective α4β2 nAChR agonist. One-photon uncaging evokes large inward currents and Ca2+transients on cell bodies and dendrites of medial habenular neurons in mouse brain slices. Two-photon uncaging induces fast nAChR-mediated currents. Photolyzed with high quantum yield of 0.20. Effective photolysis occurs using one- or two-photon excitation; one-photon uncaging requires illumination at 410 nm for 1.5-3 ms; two-photon uncaging requires illumination ...
TP2016	Huwentoxin-IV Huwentoxin IV
	Selective NaV1.7 channel blocker. Preferentially inhibits neuronal NaV1.7, 1.2 and 1.3 (IC50 values are 26, 150 and 338 nM respectively), compared to muscle subtypes NaV1.4 and 1.5 (IC50 = >10 μM). Inhibits the channel by binding at the neurotoxin recepto
T75855	Phrixotoxin 3 TFA
	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。
TP1513	Egg Laying Hormone, aplysia
	Egg-laying hormone (ELH) is a neuropeptide synthesized by the bag cell neurons, Egg-laying hormone (ELH) induces egg laying and its correlated behavior in Aplysia californica. Egg-laying hormone (ELH) has been purified to homogeneity and Egg-laying hormon
T83749	Tertiapin LQ TFA TPNLQ
	Tertiapin LQ是源自蜜蜂毒素肽tertiapin的肽衍生物，同时也是向内整流钾(Kir)通道的抑制剂。它能够抑制由G蛋白激活的向内整流钾通道1（GIRK1）和GIRK4（即Kir3.1和Kir3.4）组成的异源多聚钾通道，以及向内整流钾通道1（Kir1.1）。在活体内，tertiapin LQ抑制在雪貂中对条件刺激的Purkinje细胞暂停响应。
T69600	Spermidine-d6
	Spermidine-d6 is intended for use as an internal standard for the quantification of spermidine by GC- or LC-MS. Spermidine is an endogenous polyamine. It is formed from putrescine by spermidine synthase. Spermidine (25 µM) inhibits the activity of the human inward-rectifying potassium channel Kir2.3 in a patch-clamp assay. It induces autophagy in HeLa cells when used at a concentration of 100 µM and increases the lifespan of D. melanogaster, yeast, and C. elegans. Spermidine (30 mM in the drinki...

化合物

Cat.No: T23101

Target: Others

Cat.No: T22408

Synonym: 吡啶-3,6-二胺,3,6-Diaminoacridine

Target: Antibacterial

Proflavine Hemisulfate

Cat.No: T0438

Synonym: 3,6-Diaminoacridine hemisulfate,Proflavin hemisulfate,硫酸原黄素

Target: Others, Potassium Channel, DNA, Thrombin, Antibacterial, Autophagy

Cat.No: T4542

Synonym: Clonixic acid,氯尼辛

Target: Others

Amlodipine maleate

Cat.No: T21263

Synonym: Amlodipine (+-)-form maleate,Amvaz

Target: Calcium Channel

Cat.No: T27205

Synonym: DPI-201-106

Target: Sodium Channel

Cat.No: T36033

Synonym: NOC-18,Diethylamine NONOate

Target: NO Synthase

Cat.No: T22361

Synonym: Carbocaine

Target: Sodium Channel

Cat.No: T0866

Synonym: Rythmol,普罗帕酮,Propafenonum

Target: Potassium Channel, MRP, Sodium Channel

Ranolazine dihydrochloride

Cat.No: T0207

Synonym: 盐酸雷诺嗪,雷诺嗪二盐酸盐,RS 43285,Ranolazine 2HCl

Target: Calcium Channel, Sodium Channel, Autophagy

IK1 inhibitor PA-6

Cat.No: T15555

Target: Potassium Channel

Ibutilide Fumarate

Cat.No: T6541

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

Target: Calcium Channel, Sodium Channel

Zatebradine hydrochloride

Cat.No: T13387L

Synonym: UL-FS-49CL,UL-FS-49

Target: Others, HCN Channel

Ivabradine hydrochloride

Cat.No: T2535

Synonym: 盐酸伊伐布雷定,S 16257-2,Ivabradine HCl

Target: Adrenergic Receptor

Cat.No: T19839

Synonym: Oxatomida

Target: P2X Receptor, Calcium Channel, 5-HT Receptor, Histamine Receptor

MNI caged kainic acid

Cat.No: T23012

Target: Others

Cat.No: T24948

Synonym: VU007625,VU 625,VU 007625,VU-625,VU-007625

Cat.No: T71406

Cat.No: T5336L

Synonym: Racemic zacopride

Asocainol hydrochloride

Cat.No: T68361

Cat.No: T80510

Target: Potassium Channel

Cat.No: T70063

Cat.No: TP1967

Cat.No: T17240

Target: Others

4,9-Anhydrotetrodotoxin

Cat.No: T37093

Synonym: 4,9-Anhydrotetrodotoxin,4,9-anhydro-TTX

Cat.No: TP2114

Guanosine 5’-diphosphate (sodium salt hydrate)

Cat.No: T36740

Amlodipine mesylate

Cat.No: T63445

Cat.No: T37199

Cat.No: T70987

Cat.No: T41209

Cat.No: TP2016

Synonym: Huwentoxin IV

Phrixotoxin 3 TFA

Cat.No: T75855

Egg Laying Hormone, aplysia

Cat.No: TP1513

Tertiapin LQ TFA

Cat.No: T83749

Synonym: TPNLQ

Cat.No: T69600

Cat. No.	Product Name	Target	Signaling Pathways
T8040	Cholesterol myristate 胆甾烯基豆蔻酸酯,Cholesteryl myristate,胆固醇肉豆蔻酸,Cholesteryl tetradecanoate	Others; Potassium Channel; GABA Receptor; Endogenous Metabolite; AChR	Membrane transporter/Ion channel; Metabolism; Neuroscience; Others
	Cholesterol myristate (Cholesteryl myristate) 是粗吻海龙中的一种类固醇，可与多种离子通道结合，例如nAChR、GABAA 受体和内向整流钾离子通道。
T8195	Lotusine	Others	Others
	Lotusine 是一种提取自Nelumbo nucifera Gaertn 的绿色种胚中的纯生物碱。它能够作用于心肌中动作电位及心脏浦肯野纤维缓慢内向电流。
T78489	Lotusine hydroxide
	Lotusine (hydroxide)为纯生物碱，源自Nelumbo nucifera Gaertn绿色种胚提取。该化合物能够影响心肌动作电位和心脏浦肯野纤维的缓慢内向电流。
T74193	(R)-IDHP
	(R)-IDHP为IDHP异构体，属于丹参代谢物。该化合物能通过抑制血管平滑肌细胞电压依赖性钙通道与受体操作钙通道的Ca2+释放和Ca2+内流，发挥血管松弛作用，适用于心脑血管疾病研究。

天然产物

Cholesterol myristate

Cat.No: T8040

Synonym: 胆甾烯基豆蔻酸酯,Cholesteryl myristate,胆固醇肉豆蔻酸,Cholesteryl tetradecanoate

Target: Others, Potassium Channel, GABA Receptor, Endogenous Metabolite, AChR

Cat.No: T8195

Target: Others

Lotusine hydroxide

Cat.No: T78489

Cat.No: T74193

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