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37

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0946	Mepivacaine hydrochloride Mepivacaine HCl,盐酸甲哌卡因	Sodium Channel	Membrane transporter/Ion channel
	Mepivacaine hydrochloride (Mepivacaine HCl) 是具有局部麻醉特性的酰胺衍生物。Mepivacaine hydrochloride 与神经元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。
T8978	DD1 3,3'-Diamino-4'-methoxyflavone,HUN85111	Proteasome	Proteases/Proteasome; Ubiquitination
	DD1 (HUN85111) 是一种蛋白酶体抑制剂，可诱导人髓系肿瘤选择性凋亡。
T27794	λ-Cyhalothrin lambda-Cyhalothrin,Karate,λ-氯氟氰菊酯,Icon	Sodium Channel; Parasite	Membrane transporter/Ion channel; Microbiology/Virology
	λ-Cyhalothrin (Icon) 是广谱的 II 型合成除虫菊酯杀虫剂，含有 α-氰基，用于防治多种害虫。它是一种钠通道神经毒素，靶向中枢神经系统中神经元膜。
T2525	Alosetron hydrochloride Lotronex,盐酸阿洛司琼,GR 68755C,GR 68755,GR 68755X	5-HT Receptor	GPCR/G Protein; Neuroscience
	Alosetron hydrochloride (GR 68755) 是一种高选择性的 5-HT3 受体拮抗剂，可减轻清醒或麻醉犬直肠扩张的内脏伤害性效应，具有抗炎活性，用于肠易激综合征的研究。它阻断 5HT3 介导的豚鼠肌间和粘膜下神经元的快速去极化，IC50约为 55 nM。
T0030	Bupivacaine hydrochloride Vivacaine,Bupivacaine HCl,盐酸布比卡因	Sodium Channel	Membrane transporter/Ion channel
	Bupivacaine hydrochloride (Vivacaine) 是NMDA 受体抑制剂，可用于慢性疼痛的研究。它可阻断钠、L-钙和钾通道，还阻断SCN5A 通道，IC50为 69.5 μM。
T0018	Procainamide hydrochloride Procapan,Procainamide HCl,Pronestyl,Procanbid,盐酸普鲁卡因胺	DNA Methyltransferase; Sodium Channel; AChR; Autophagy	Autophagy; Chromatin/Epigenetic; Membrane transporter/Ion channel; Neuroscience
	Procainamide hydrochloride (Procapan) 是一种用于研究心律失常的抗心律失常制剂。
T30249	AZD 7009 AZD-7009,AZD7009	Sodium Channel	Membrane transporter/Ion channel
	AZD 7009是一种新型抗心律失常化合物，对CHO K1细胞中 hNav1.5的钠电流具有抑制作用，IC50为11 uM。AZD 7009 对离体兔心房和心室肌细胞的晚期钠电流具有抑制作用，对e -4031诱导的动作电位持续时间延长具有抑制作用，促使浦肯野纤维的早期后去极化(EADs)。
T64394	GW 833972A	Cannabinoid Receptor	GPCR/G Protein
	GW 833972A 是一种选择性的 CB2 受体激动剂。GW 833972A 对诱导神经去极化具有抑制作用，且在动物模型中对柠檬酸引起的咳嗽具有抑制作用。
T7502L	PF 05089771 PF-05089771,PF05089771	Sodium Channel	Membrane transporter/Ion channel
	PF 05089771是具有口服有效的、选择性的 Nav1.7丙烯酰胺抑制剂。PF-05089771在疼痛和糖尿病神经性疾病的研究中具有价值。
T1320	Disopyramide Triombrin,Hypaque sodium,amidotrizoate sodium,达舒平	Potassium Channel; Sodium Channel; AChR	Membrane transporter/Ion channel; Neuroscience
	Disopyramide (Triombrin) 是用于研究房性和室性心律失常的 IA 类抗心律失常试剂。它阻断心肌快速内向钠电流，延长心肌动作电位持续时间。它抑制 HERG 编码的钾通道。它也表现出复杂的蛋白质结合，并具有强大的负性肌力作用。
T10706	CCI-006	Mitochondrial Metabolism	Metabolism
	CCI-006 是一种 MLL 重排白血病细胞的选择性抑制剂和化学增敏剂。它能够抑制线粒体呼吸，造成 MLL-r 白血病细胞亚群中无法克服的线粒体去极化和促凋亡未折叠蛋白反应。
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。
T35689	MTP 131 acetate	Others	Others
	MTP 131 acetate 是一种小的线粒体靶向四肽。
T68904	GW-833972A free base
	GW833972 is a CB2 Agonist. GW 833972A inhibited capsaicin-induced depolarization of the human and guinea-pig and prostaglandin E(2) (PGE(2)) and hypertonic saline-induced depolarization of the guinea-pig isolated vagus nerve in vitro. GW 833972A also inhibited citric acid-induced cough but not plasma extravasation in the guinea-pig and this effect was blocked by a CB(2) receptor antagonist.
T61215	Alinidine hydrobromide
	Alinidine hydrobromide, a specific bradycardic agent, diminishes the slope of the diastolic depolarization in sinoatrial tissue and Purkinje fibers [1].
T26573	AG311 AG 311,AG-311
	AG311 is an inhibitor of complex I and hypoxia-induced HIF-1α stabilization. In vitro, AG311 induces rapid necrosis in numerous cancer cell lines. Within minutes, exposure to AG311 also results in mitochondrial depolarization, superoxide production, and i
T28562	Ro 18-3981 Ro-18-3981,Ro 183981
	Ro 18-3981 is an inhibition of myocardial Ca2+ channels. The KD value of Ro 18-3981 (1.0 nM) was similar to the IC50 value for blockade of ICa at a Vh of -20 mV (2.3 nM), i.e. at a level of near-maximal depolarization.
T25934	Pentisomide Pentisomidum
	Pentisomide 是一种抗心律失常的化合物，对去极化（Ia 和 Ic 类作用）和复极有显著作用。它可剂量依赖性地抑制缺血再灌注心律失常。Pentisomide 已进入治疗心律失常的 II 期临床试验。
T37748	Ivermectin B1b
	Ivermectin B1b is the minor component . It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function.
T83220	a-Bag Cell Peptide (1-8)
	α-Bag Cell Peptide (1-8)为α-bag cell peptide的NH2末端片段，能够抑制左上象限(LUQ)神经元活动，并防止袋细胞去极化。
T76453	Substance P (6-11)
	Substance P (6-11)，Substance P 的C末端六肽酰胺，可与NK-1速激肽受体结合，展现出对运动神经元的去极化作用以及降压效应。
T27032	CK59 CK-59,CK 59
	CK59 is a reversible inhibitor of calcium-calmodulin-dependent kinase II (CaMKII). CK59 inhibits multiple voltage-gated calcium channels, including the L-type channel during depolarization in a dose-dependent manner. The IC50 for CK59 was approximately 50
T83221	a-Bag Cell Peptide (1-7)
	α-Bag Cell Peptide (1-7)是α-bag cell peptide的NH2末端片段，具有抑制左上象限(LUQ)神经元及阻止袋细胞去极化的功能。
T80455	ω-Conotoxin CVIB	Sodium Channel	Membrane transporter/Ion channel
	ω-Conotoxin CVIB为非选择性N型及P/Q型电压门控钙通道(VGCC)拮抗剂，能够抑制背根神经节(DRG)中神经元去极化后激活全细胞VGCC电流，其pIC50值为7.64。
T62217	Tubulin polymerization-IN-9
	Tubulin polymerization-IN-9 是一种微管蛋白 (tubulin) 的有效抑制剂 (IC50: 1.82 μM)。Tubulin polymerization-IN-9 能够将 K562 细胞的细胞周期停滞在 G2/M 期，并诱导其凋亡 (apoptosis) 及线粒体去极化。Tubulin polymerization-IN-9 表现出强大的抗血管和抗肿瘤作用。
T80457	ω-Conotoxin Bu8	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	ω-Conotoxin Bu8为含25个氨基酸残基和3个二硫键的ω-芋螺毒素。该化合物能选择性地抑制HEK293T细胞内表达的大鼠CaV2.2介导的Ba2+去极化激活电流，表现出高效的IC50值为89 nM。
T80282	cPcAMP1/26
	cPcAMP1/26 是一款抗菌肽，能高效清除A.Hydrophila及金黄色葡萄球菌 (S. aureus)。该化合物通过诱导细菌质膜去极化作用并提升细胞内ROS水平，展示其抗菌机制。
T37201	CAY10787
	CAY10787 is an oxysterol and a negative allosteric modulator of GABAAreceptors.1,2It reduces GABA-induced currents in HEK cells expressing α1β1γ2or α4β3γ2subunit-containing GABAAreceptors (IC50s = 1.5 and 1 μM, respectively).2CAY10787 (500 nM) reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.In vivo, CAY10787 (2, 10, and 50 mg/kg) increases latency to nocifensive behaviors in t...
T80495	mHuwentoxin-IV	Sodium Channel	Membrane transporter/Ion channel
	mHuwentoxin-IV是一种经天然修饰的Huwentoxin-IV。该化合物针对背根神经节中河豚毒素敏感(TTX-S)电压门控钠通道(sodium channels)表现出抑制作用，IC50值为54.16 nM。mHuwentoxin-IV对这些钠通道的抑制作用并不会因强去极化电压而逆转。
T37469	Sitamaquine tosylate
	Sitamaquine is an antileishmanial agent.1It is active againstL. donovani,L. infantum,L. mexicana,L. braziliensis, andL. tropica(EC50s = 9.5-19.8 μM). It inhibits mitochondrial complex II, also known as succinate dehydrogenase (SDH), in a cell-free assay when used at concentrations ranging from 10 to 200 μM.2Sitamaquine (100 μM) increases intracellular levels of reactive oxygen species (ROS) and decreases intracellular ATP levels, as well as induces phosphatidylserine externalization, chromatin f...
T82546	DiSBAC10
	DiSBAC10是一种电压敏感荧光探针，用于FRET检测中研究细胞膜的电活动。在静息极化的细胞中，DiSBAC10位于膜的外leaflet，从激发的荧光素标记蛋白那里接收光子，并以更高的波长重新发射光子。当细胞去极化时，DiSBAC10迅速转移到膜的内leaflet，从而增加了荧光团之间的距离并减少FRET信号。
T38204	GAT229
	GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 an...
T75074	6-Methoxypurine-9-β-D-5’(R)-C-methylriboside
	6-Methoxypurine-9-β-D-5’(R)-C-methylriboside 是一种嘌呤碱基，属于次黄嘌呤似物，主要在肌肉组织中发现。作为黄嘌呤在嘌呤氧化酶作用下的代谢产物，次黄嘌呤具备显著的抗炎性质，并可作为内源性 poly(ADP-ribose) polymerase (PARP) 的抑制剂。其通过抑制 PARP 活性，防止过氧亚硝酸盐引起的线粒体去极化及次级超氧化物的产生，展现出细胞保护作用。同时，次黄嘌呤也被用作缺氧的生物标志物。
T83891	Sulfonadyn-47
	Sulfonadyn-47是一种dynamin抑制剂，能在无细胞测定中抑制dynamin的GTP酶活性（IC50 = 3.5 µM）。在U2OS细胞中，Sulfonadyn-47抑制clathrin介导的内吞作用（IC50 = 27.3 µM），同时在分离的大鼠脑突触体中抑制由去极化刺激的FM4-64摄取，后者是突触小泡内吞（SVE）的标志（IC50 = 12.3 µM）。在体内，Sulfonadyn-47（30和60 mg/kg）在6 Hz角膜电引发小鼠癫痫模型中具有抗惊厥活性。
T36521	Alaproclate (hydrochloride)
	Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentratio...
T37297	Ru360
	Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial ce...
T83735	Pap12-6 TFA
	Pap12-6是一种从蝶类P. xuthus幼虫中发现的papiliocin十二个N-端氨基酸衍生的抗菌肽。它对包括E. coli、P. aeruginosa和S. syphimurium在内的八种革兰氏阴性细菌（MIC50s = 4-8 µM）以及革兰氏阳性细菌S. aureus、耐甲氧西林的S. aureus 3126（MRSA-3126）、B. subtilis和S. epidermidis（MIC50s = 4-8 µM）具有活性，但在25 µM浓度下不影响人类红细胞、小鼠RAW 264.7巨噬细胞、人类HaCaT角质形成细胞或人类HEK293肾细胞的活性。Pap12-6在4和8 µM浓度下可引起E. coli的膜去极化。Pap12-6（10 µM）预处理可降低LPS刺激的RAW 264.7巨噬细胞中一氧化氮（NO2-）、Tnf-α和Il-6的分泌水平。在体内，Pap12-6（10 mg/kg）可以提高感染E. coli的小鼠的存活率，并且在剂量为1 mg/kg时减少感染E. coli小鼠的肺、肝和肾中菌落形成单位（CFUs）的数量。Pap12-6（1 mg/kg）在E. co...

化合物

Mepivacaine hydrochloride

Cat.No: T0946

Synonym: Mepivacaine HCl,盐酸甲哌卡因

Target: Sodium Channel

Cat.No: T8978

Synonym: 3,3'-Diamino-4'-methoxyflavone,HUN85111

Target: Proteasome

Cat.No: T27794

Synonym: lambda-Cyhalothrin,Karate,λ-氯氟氰菊酯,Icon

Target: Sodium Channel, Parasite

Alosetron hydrochloride

Cat.No: T2525

Synonym: Lotronex,盐酸阿洛司琼,GR 68755C,GR 68755,GR 68755X

Target: 5-HT Receptor

Bupivacaine hydrochloride

Cat.No: T0030

Synonym: Vivacaine,Bupivacaine HCl,盐酸布比卡因

Target: Sodium Channel

Procainamide hydrochloride

Cat.No: T0018

Synonym: Procapan,Procainamide HCl,Pronestyl,Procanbid,盐酸普鲁卡因胺

Target: DNA Methyltransferase, Sodium Channel, AChR, Autophagy

Cat.No: T30249

Synonym: AZD-7009,AZD7009

Target: Sodium Channel

Cat.No: T64394

Target: Cannabinoid Receptor

Cat.No: T7502L

Synonym: PF-05089771,PF05089771

Target: Sodium Channel

Cat.No: T1320

Synonym: Triombrin,Hypaque sodium,amidotrizoate sodium,达舒平

Target: Potassium Channel, Sodium Channel, AChR

Cat.No: T10706

Target: Mitochondrial Metabolism

Ivabradine hydrochloride

Cat.No: T2535

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

Target: Adrenergic Receptor

MTP 131 acetate

Cat.No: T35689

Target: Others

GW-833972A free base

Cat.No: T68904

Alinidine hydrobromide

Cat.No: T61215

Cat.No: T26573

Synonym: AG 311,AG-311

Cat.No: T28562

Synonym: Ro-18-3981,Ro 183981

Cat.No: T25934

Synonym: Pentisomidum

Cat.No: T37748

a-Bag Cell Peptide (1-8)

Cat.No: T83220

Substance P (6-11)

Cat.No: T76453

Cat.No: T27032

Synonym: CK-59,CK 59

a-Bag Cell Peptide (1-7)

Cat.No: T83221

ω-Conotoxin CVIB

Cat.No: T80455

Target: Sodium Channel

Tubulin polymerization-IN-9

Cat.No: T62217

ω-Conotoxin Bu8

Cat.No: T80457

Target: Calcium Channel

Cat.No: T80282

Cat.No: T37201

Cat.No: T80495

Target: Sodium Channel

Sitamaquine tosylate

Cat.No: T37469

Cat.No: T82546

Cat.No: T38204

6-Methoxypurine-9-β-D-5’(R)-C-methylriboside

Cat.No: T75074

Cat.No: T83891

Alaproclate (hydrochloride)

Cat.No: T36521

Cat.No: T37297

Cat.No: T83735

Cat. No.	Product Name	Target	Signaling Pathways
T0508	γ-Aminobutyric acid Gamma-aminobutyric acid,4-Aminobutyric acid,4-氨基丁酸,γ-氨基丁酸,GABA,4-Aminobutanoic acid,Piperidic acid	GABA Receptor; Endogenous Metabolite	Membrane transporter/Ion channel; Metabolism; Neuroscience
	γ-Aminobutyric acid (4-Aminobutyric acid) 是成年哺乳动物大脑中主要的抑制性神经递质，能够与离子移变 GABA 受体(GABAA) 受体和促代谢受体 (GABAB) 受体结合发挥作用。
T7995	α-Angelica lactone α-当归内酯,当归内酯,Alpha-Angelica Lactone	Others; GST	Others; oxidation-reduction
	α-Angelica lactone 是一种乙烯基亲核试剂，也是一种天然存在的抗癌剂。它可以得到手性的 δ-氨基 γ，γ-二取代丁烯醇内酯羰基衍生物，并在 γ-碳上表现出亲电子俘获。它通过选择性增强谷胱甘肽-S-硫转移酶 (GST) 和 UDP-葡糖苷转移酶 (UGT) 解毒酶发挥强大的化学保护作用。
T4S1876	3-Deoxyaconitine	Sodium Channel	Membrane transporter/Ion channel
	3-Deoxyaconitine 是一种二萜类生物碱，对钠离子通道有激活作用。
T13701	Genistein 8-c-glucoside G8CG	Mitochondrial Metabolism	Metabolism
	Genistein 8-c-glucoside (G8CG) 诱导线粒体膜去极化从而导致细胞凋亡。Genistein 8-c-glucoside 是一种来源于 Lupinus luteus L.花中的天然葡萄糖苷。
T27564	Hymenidin	5-HT Receptor	GPCR/G Protein; Neuroscience
	Hymenidin是一种从冲绳海绵Hymeniacidon sp。中分离出的生物碱，是一种5-羟色胺能受体拮抗剂和电压门控钾通道抑制剂，具有潜在的抗原生动物作用，可选择性结合 FOXO1 DNA ，可降低去极化诱导的细胞钙升高。

天然产物

γ-Aminobutyric acid

Cat.No: T0508

Synonym: Gamma-aminobutyric acid,4-Aminobutyric acid,4-氨基丁酸,γ-氨基丁酸,GABA,4-Aminobutanoic acid,Piperidic acid

Target: GABA Receptor, Endogenous Metabolite

α-Angelica lactone

Cat.No: T7995

Synonym: α-当归内酯,当归内酯,Alpha-Angelica Lactone

Target: Others, GST

3-Deoxyaconitine

Cat.No: T4S1876

Target: Sodium Channel

Genistein 8-c-glucoside

Cat.No: T13701

Synonym: G8CG

Target: Mitochondrial Metabolism

Cat.No: T27564

Target: 5-HT Receptor

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