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63

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1765	Erastin	Ferroptosis; VDAC	Apoptosis; Membrane transporter/Ion channel
	Erastin 是一种作用于线粒体 VDAC 的铁死亡激活剂，具有 ROS 和铁依赖性。Erastin 具有抗肿瘤活性，选择性作用于 RAS 致癌突变的肿瘤细胞。该产品在溶液中不稳定，建议现配现用。
T3572	NSC 15364 1,3-Bis(4-aminophenyl)urea,NSC15364	Apoptosis; Others; VDAC	Apoptosis; Membrane transporter/Ion channel; Others
	NSC 15364 (1,3-Bis(4-aminophenyl)urea) 是一种 VDAC1寡聚化和细胞凋亡抑制剂。
T18975	DIDS sodium salt 4,4'-二异硫氰酸基-2,2'-二苯乙烯磺酸二钠[蛋白质改性试剂],MDL101114ZA	VDAC; ABC	Membrane transporter/Ion channel
	DIDS sodium salt (MDL101114ZA) 是有效的ABCA1和VDAC1双抑制剂。
T2141	Mecamylamine hydrochloride 盐酸美加明,Inversine,Mevasin	AChR	Neuroscience
	Mecamylamine hydrochloride (Mevasin) 是一种易穿过血脑屏障的烟碱拮抗剂，用作高血压的神经节阻滞剂，具有抗神经疾病作用。
T0825	Ebselen SPI-1005,PZ-51,依布硒,CCG-39161	Phosphatase; Virus Protease; Calcium Channel; COX; HIV Protease	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Ebselen (CCG-39161) 是一种谷胱甘肽过氧化物酶模拟物，是电压依赖性钙通道阻断剂。它抑制Mpro 和COVID-19病毒，是HIV-1衣壳 CTD 二聚化的抑制剂，具有抗炎、抗癌和抗氧化活性。
T16887	Sipatrigine 619C89,BW 619C89	Calcium Channel; Sodium Channel	Membrane transporter/Ion channel; Metabolism
	Sipatrigine is a glutamate release inhibitor and voltage-dependent sodium channel.
T20341	DNDS	CFTR	Membrane transporter/Ion channel
	DNDS 是电压依赖性囊性纤维化跨膜电导调节剂 (CFTR) 的通道阻滞剂。
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。
T13428	(5R)-BW-4030W92	Sodium Channel	Membrane transporter/Ion channel
	(5R)-BW-4030W92是 R 型的 BW-4030W92 ，是具有活性的对映体。(5R)-BW-4030W92 是一种可口服的非选择性、电压依赖性和使用依赖性的钠离子通道 (sodium channel) 拮抗剂，可用于研究神经系统疾病。
T17227	Vernakalant Hydrochloride RSD1235 hydrochloride	Potassium Channel; Sodium Channel	Membrane transporter/Ion channel
	Vernakalant Hydrochloride (RSD1235 hydrochloride) 是一种混合电压和频率依赖性的 Na+ 和 K+ 通道阻断剂。Vernakalant 抑制 Kv1.5 channelwt，Kv1.5 channelI508F，Kv1.5 channelT479A，IC50 分别为 13.35±0.93 μM。
T0596	Phenylhydantoin 5-苯基海因,5-Phenylhydantoin	Others	Others
	Phenylhydantoin (5-Phenylhydantoin) 是 Mephenytoin 的代谢物。它已被证明与电压依赖性钠通道 (NVSC) 结合并具有抗癫痫特性。
T30188L	Atagabalin HCl PD-0200390 HCl,Atagabalin HCl(223445-75-8 Free base）	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Atagabalin HCl 是一种新型电压依赖性钙通道（VDCC）α2δ亚基（1 和 2）配体，会影响慢波睡眠,可用于治疗失眠。
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。
T26778L	Besipirdine hydrochloride HP 749 hydrochloride,Besipirdine hydrochloride（119257-34-0 Free base)	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Besipirdine hydrochloride 是一种非受体依赖性拟胆碱化合物，具有α-肾上腺素能活性和心血管活性。Besipirdine hydrochloride 抑制电压依赖性钠钾通道，抑制生物胺的摄取。Besipirdine hydrochloride 可减少大鼠的时间表诱导的烦渴，增强中枢神经系统中的胆碱能和肾上腺素能神经传递。
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。
T13287	VBIT-4	VDAC	Membrane transporter/Ion channel
	VBIT-4 是一种电压依赖性阴离子通道 1 (VDAC1) 寡聚化抑制剂（Kd：17 μM）。 VBIT-4 可用于治疗凋亡相关疾病（如神经退行性疾病和心血管疾病）。
T26778	Besipirdine HP 749 free base,P-867493,P867493,HP 749,HP749,P 867493	Sodium Channel; Adrenergic Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Besipirdine (HP 749 free base)是一种非受体依赖性拟胆碱化合物，具有α-肾上腺素能活性和心血管活性。Besipirdine 抑制电压依赖性钠钾通道，抑制生物胺的摄取。Besipirdine 可减少大鼠的时间表诱导的烦渴，增强中枢神经系统中的胆碱能和肾上腺素能神经传递。
T68060	Elgodipine
	Elgodipine 显著降低了运动诱导的心绞痛系统的发生率和严重程度，能够通过独立于转录因子c-fos 和c-jun 表达的机制抑制血管平滑肌增殖。 Elgodipine 诱导的抑制是电压依赖性的。Elgodipine 是治疗心绞痛的潜在化合物。
T40376	L-Phenylalanine-15N L-苯丙氨酸 15N,(S)-2-Amino-3-phenylpropionic acid-15N,L-Phenylalanine-15N	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	L-Phenylalanine-15N ((S)-2-Amino-3-phenylpropionic acid-15N) 是 15N 标记的 L-Phenylalanine。L-Phenylalanine 是从大肠杆菌中分离出来的一种必需氨基酸。 L-Phenylalanine 广泛用于食品香精和药物的生产。
T23274	RuBi-4AP	Others	Others
	voltage-dependent K+ channel blocker
T70199	Enecadin HCl
	Enecadin HCl is a voltage-dependent sodium and calcium channel blocker.
T26092	Risotilide
	Risotilide is a voltage-dependent potassium channel inhibitor. It can prolong cardiac action potentials and refractory periods.
T16487	PF-05241328	Others	Others
	PF-05241328 is an effective and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (IC50: 31 nM).
T16447	β-Amino Acid Imagabalin Hydrochloride PD-0332334	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	β-Amino Acid Imagabalin Hydrochloride is the voltage-dependent calcium channel ligand for the α2δ subunit.
T36808	UK 59811 hydrochloride
	Blocks CaVAb, a site-directed mutant of bacterial NaVAb with full voltage-dependent Ca2+ channel function (IC50 = 194 nM). Tang et al (2016) Structural basis for inhibition of a voltage-gated Ca2+ channel by Ca2+ antagonist drugs. Nature 537 117 PMID:27556947
T71281	Nerispirdine
	Nerispirdine is a biochemical that inhibits batrachotoxin binding to voltage-dependent sodium channels.
T19788	Piretanide Eurelix,Tauliz,Arelix
	Piretanide is a time- and voltage-dependent blocker of CFTR Cl(-) currents. Piretanide also acts as a loop diuretic.
T10209	A-887826	Others	Others
	A-887826 is a selective, orally bioavailable, and voltage-dependent Na(v1.8) channel blocker (IC50: 11 nM). It attenuates neuropathic tactile allodynia in vivo.
T80439	GTx1-15	Sodium Channel	Membrane transporter/Ion channel
	GTx1-15为一种抑制剂胱氨酸结 (ICK) 肽，能有效抑制电压依赖性钙通道 Cav3.1 以及电压依赖性钠通道 Nav1.3 和 Nav1.7。
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.
T70691	ITP-2
	ITP-2 is a selective activator of hERG channels. ITP-2 causes large depolarizing shifts in the midpoint of voltage-dependent inactivation and hyperpolarizing shifts in the voltage-dependence of activation.
TP2118	SNX-482 SNX 482
	Potent and selective, voltage-dependent R-type CaV2.3 calcium channel blocker (IC50 = 30 nM). Antinociceptive; inhibits nociceptive C-fibre and Aδ-fibre-evoked neuronal responses.
T68125	(Rac)-PD0299685 (Rac)-PF-299685	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	(Rac)-PD0299685 是一种有效的电压依赖性钙通道抑制剂，可用于研究视网膜相关疾病。
T28346	PD-217014 HCl PD 217014,PD217014,PD-217,014,PD-217014
	PD-217014 is a GABA analog. It inhibits (3)H-gabapentin binding to alpha(2)delta subunit of voltage-gated calcium channels in a concentration-dependent manner (K(i) = 18 nmol/l). PD-217014 possesses visceral analgesic activity.
T23210	Quinacrine (dihydrochloride hydrate) Quinacrine (hydrochloride hydrate) (83-89-6 free base)	Others	Others
	Quinacrine is a compound that is commonly used as an anti-protozoal agent. It inhibits voltage-dependent sodium channels (IC50: 3.3 μM） and suppresses aldehyde oxidase (IC50: 3.3 μM). Quinacrine prevents misfolding of prion protein (EC50: 0.3 μM). As an e
T19591	Triamterene D5 氨苯蝶啶 D5	Others	Others
	Triamterene D5 is a deuterium-labeled Triamterene and can block epithelial Na+ channel (ENaC) in a voltage-dependent manner, used as a mild diuretic.
T26564	ADCI SGB-017,SGB017,SGB 017
	ADCI is an inhibitor of voltage-activated sodium channels and N-methyl-D-aspartate (NMDA)-receptor-gated channels. Inhibition of sodium channels by ADCI was voltage dependent. High doses of ADCI increased dopamine metabolism in the prefrontal cortex and/o
T14150	AKOS-22	Others	Others
	AKOS-22 is a potent mitochondrial protein VDAC1 (voltage-dependent anion channel 1) inhibitor (Kd=15.4 μM). AKOS-22 protects against mitochondrial dysfunction[1]. AKOS-22 interacts with VDAC1 and inhibiting both VDAC1 oligomerization and apoptosis.
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
T80184	GsAF-II	Sodium Channel	Membrane transporter/Ion channel
	GsAF-II，一种肽毒素，能电压依赖性阻断hERG1亚型钾通道，并对Nav1.x亚型钠离子通道展现阻断效应。
T76392	β-Bag cell peptide
	β-Bag cell peptide是一种提高袋细胞神经元(bag cell neuron)中cAMP水平、并能降低电压依赖性钾电流的神经活性肽。
T13286	VBIT-3	Others	Others
	VBIT-3 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 31.3 μM). VBIT-3 also is an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).
T28160	Nerispirdine HCl HP-184,HP 184,Nerispirdine hydrochloride,HP184
	Nerispirdine is a acetylcholine release enhancer, sodium channel blocker and K(V) 2.1 channel blocker. Nerispirdine inhibits voltage-dependent Na(+) channel currents recorded from human SH-SY5Y cells with an IC(50) of 11.9 micromol/L when measured from a
T68918	Phenytoin-d10
	Phenytoin-d10 is intended for use as an internal standard for the quantification of phenytoin by GC- or LC-MS. Phenytoin is an anticonvulsant agent and active metabolite of fosphenytoin. Phenytoin is formed from fosphenytoin by tissue phosphatases. It inhibits neuronal voltage-gated sodium channels in a voltage-dependent manner. Phenytoin reduces the neuronal firing frequency and decreases the amplitude of excitatory post-synaptic potentials (EPSPs) in electrically stimulated rat corticostriatal...
T80434	Heteropodatoxin-2	Potassium Channel	Membrane transporter/Ion channel
	Heteropodatoxin-2为含30个氨基酸的肽，归属于异足毒素类。它能电压依赖性地阻断非洲爪蟾卵母细胞表达的Kv4.2电流，并在正电位较高时显示出较低的阻断效应。
T23652	AFD-21 AFD21,NS-2 Class 1 antiarrhythmic agent
	AFD-21是一种 I 类抗心律失常药物。它在钠通道失活状态下与钠通道结合，对钠通道具有使用和电压依赖性抑制作用，其解结合率与具有中等动力学的I 类抗心律失常药物相当。
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。
T60306	NMDA receptor antagonist 4
	NMDA receptor antagonist 4 (IIc) 是一个非竞争性、电压依赖的、口服活性的 NMDAR 阻断剂，IC50值为1.93 μM。NMDA receptor antagonist 4 可透过血脑屏障，可用于研究阿兹海默症。
T11240	Ethacrynic acid D5	Others	Others
	Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by...
T80028	Iberiotoxin TFA	Potassium Channel	Membrane transporter/Ion channel
	Iberiotoxin (TFA) 是选择性高电导率Ca2+-activated K+ channel抑制剂，Kd约1 nM，不干扰其他电压依赖性离子通道。

化合物

Cat.No: T1765

Target: Ferroptosis, VDAC

Cat.No: T3572

Synonym: 1,3-Bis(4-aminophenyl)urea,NSC15364

Target: Apoptosis, Others, VDAC

DIDS sodium salt

Cat.No: T18975

Synonym: 4,4'-二异硫氰酸基-2,2'-二苯乙烯磺酸二钠[蛋白质改性试剂],MDL101114ZA

Target: VDAC, ABC

Mecamylamine hydrochloride

Cat.No: T2141

Synonym: 盐酸美加明,Inversine,Mevasin

Target: AChR

Cat.No: T0825

Synonym: SPI-1005,PZ-51,依布硒,CCG-39161

Target: Phosphatase, Virus Protease, Calcium Channel, COX, HIV Protease

Cat.No: T16887

Synonym: 619C89,BW 619C89

Target: Calcium Channel, Sodium Channel

Cat.No: T20341

Target: CFTR

Amlodipine maleate

Cat.No: T21263

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

Target: Calcium Channel

(5R)-BW-4030W92

Cat.No: T13428

Target: Sodium Channel

Vernakalant Hydrochloride

Cat.No: T17227

Synonym: RSD1235 hydrochloride

Target: Potassium Channel, Sodium Channel

Phenylhydantoin

Cat.No: T0596

Synonym: 5-苯基海因,5-Phenylhydantoin

Target: Others

Cat.No: T30188L

Synonym: PD-0200390 HCl,Atagabalin HCl(223445-75-8 Free base）

Target: Calcium Channel

Cat.No: T7502L

Synonym: PF-05089771,PF05089771

Target: Sodium Channel

Besipirdine hydrochloride

Cat.No: T26778L

Synonym: HP 749 hydrochloride,Besipirdine hydrochloride（119257-34-0 Free base)

Target: Adrenergic Receptor

Bupivacaine hydrochloride

Cat.No: T0030

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

Target: Sodium Channel

Cat.No: T13287

Target: VDAC

Cat.No: T26778

Synonym: HP 749 free base,P-867493,P867493,HP 749,HP749,P 867493

Target: Sodium Channel, Adrenergic Receptor

Cat.No: T68060

L-Phenylalanine-15N

Cat.No: T40376

Synonym: L-苯丙氨酸 15N,(S)-2-Amino-3-phenylpropionic acid-15N,L-Phenylalanine-15N

Target: Calcium Channel

Cat.No: T23274

Target: Others

Cat.No: T70199

Cat.No: T26092

Cat.No: T16487

Target: Others

β-Amino Acid Imagabalin Hydrochloride

Cat.No: T16447

Synonym: PD-0332334

Target: Calcium Channel

UK 59811 hydrochloride

Cat.No: T36808

Cat.No: T71281

Cat.No: T19788

Synonym: Eurelix,Tauliz,Arelix

Cat.No: T10209

Target: Others

Cat.No: T80439

Target: Sodium Channel

Cat.No: TP1967

Cat.No: T70691

Cat.No: TP2118

Synonym: SNX 482

(Rac)-PD0299685

Cat.No: T68125

Synonym: (Rac)-PF-299685

Target: Calcium Channel

Cat.No: T28346

Synonym: PD 217014,PD217014,PD-217,014,PD-217014

Quinacrine (dihydrochloride hydrate)

Cat.No: T23210

Synonym: Quinacrine (hydrochloride hydrate) (83-89-6 free base)

Target: Others

Cat.No: T19591

Synonym: 氨苯蝶啶 D5

Target: Others

Cat.No: T26564

Synonym: SGB-017,SGB017,SGB 017

Cat.No: T14150

Target: Others

Cat.No: T27032

Synonym: CK-59,CK 59

Cat.No: T80184

Target: Sodium Channel

β-Bag cell peptide

Cat.No: T76392

Cat.No: T13286

Target: Others

Nerispirdine HCl

Cat.No: T28160

Synonym: HP-184,HP 184,Nerispirdine hydrochloride,HP184

Cat.No: T68918

Heteropodatoxin-2

Cat.No: T80434

Target: Potassium Channel

Cat.No: T23652

Synonym: AFD21,NS-2 Class 1 antiarrhythmic agent

Tityustoxin-Kα

Cat.No: T80980

Synonym: TsTx-Kα

NMDA receptor antagonist 4

Cat.No: T60306

Ethacrynic acid D5

Cat.No: T11240

Target: Others

Iberiotoxin TFA

Cat.No: T80028

Target: Potassium Channel

Cat. No.	Product Name	Target	Signaling Pathways
T3377	L-Phenylalanine L-苯丙氨酸,(S)-2-Amino-3-phenylpropionic acid,phenylalanine,3-Phenyl-L-alanine	Calcium Channel; Endogenous Metabolite; iGluR	Membrane transporter/Ion channel; Metabolism; Neuroscience
	L-Phenylalanine (3-Phenyl-L-alanine) 是分离自大肠杆菌的必需氨基酸，是 NMDARs(KB573 μM) 和非 NMDARs 的甘氨酸和谷氨酸结合位点的竞争性拮抗剂，用于食品香料和药品的生产中。它是一种电压依赖性 α2δ 亚基 Ca2+通道拮抗剂，Ki 为 980 nM。
TN1121	Evocarpine	Apoptosis; cAMP; Anti-infection; Calcium Channel; Antibacterial	Apoptosis; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology
	Evocarpine 是从 Evodiae fructus 分离得到的一种喹诺酮类生物碱，有抗细菌活性。它可通过电压依赖性钙通道抑制 Ca2+内流。
TN4183	Hardwickiic acid (-)-Hardwikiic acid	Sodium Channel	Membrane transporter/Ion channel
	Hardwickiic acid ((-)-Hardwikiic acid) 是一种从Pulicaria gnaphalodes 中提取的天然化合物，是一种抗伤害性感受作用化合物。Hardwickiic acid 能阻断河豚毒素敏感的电压依赖性钠通道 (sodium channels)。Hardwickiic acid 具有抗炎和杀虫活性。
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。
TN2534	1-Hydroxy-2,3,5-trimethoxyxanthone	IκB/IKK; Calcium Channel; NOS; 5-HT Receptor; COX	GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB
	1-Hydroxy-2,3,5-trimethoxyxanthone (HM-1) has vasodilator action ,which involves both an endothelium-dependent mechanism involving NO and an endothelium-independent mechanism by inhibiting Ca(2+) influx through L-type voltage-operated Ca(2+) channels; a minor contribution to the effects of HM-1 may be related to inhibition of the protein kinase C-mediated release of intracellular Ca(2+) stores. HM-1,at the concentration of 1 ug/mL, can effectively inhibit the osteoclast differentiation in a co-c...

天然产物

L-Phenylalanine

Cat.No: T3377

Synonym: L-苯丙氨酸,(S)-2-Amino-3-phenylpropionic acid,phenylalanine,3-Phenyl-L-alanine

Target: Calcium Channel, Endogenous Metabolite, iGluR

Cat.No: TN1121

Target: Apoptosis, cAMP, Anti-infection, Calcium Channel, Antibacterial

Hardwickiic acid

Cat.No: TN4183

Synonym: (-)-Hardwikiic acid

Target: Sodium Channel

Cat.No: T74193

1-Hydroxy-2,3,5-trimethoxyxanthone

Cat.No: TN2534

Target: IκB/IKK, Calcium Channel, NOS, 5-HT Receptor, COX

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