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24

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22514	4F 4PP oxalate	5-HT Receptor	GPCR/G Protein; Neuroscience
	4F 4PP oxalate 是一种选择性5-HT2A 拮抗剂。
T3478	Ro 67-7476	GluR	Neuroscience
	Ro 67-7476 是mGluR1的正变位调节剂，能增强表达 rat mGluR1a 的 HEK293 细胞中谷氨酸诱导的钙释放，EC50为 60.1 nM。它是 P-ERK1/2 激动剂，可以在外源添加谷氨酸的情况下激活 ERK1/2 磷酸化 (EC50=163.3 nM)。
T17197	UCL 2077
	UCL 2077 是癫痫相关 KCNQ 通道的亚型选择性阻滞剂，也是一种选择性慢后超极化通道阻滞剂，在培养的海马神经元中 IC50 为 500 nM，对 Ca2+ 通道、动作电位、输入电阻的影响小，以及超极化后的介质。
T38192	Unifiram	Others	Others
	Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。
T4440	Saclofen	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Saclofen 是竞争性GABAB 受体拮抗剂(IC50:7.8 μM)。它可研究 GABAB 受体调节大脑中缓慢抑制性突触后电位的功能。
T8944	TTA-A2	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	TTA-A2 是一种选择性 T 型钙通道拮抗剂，是一种有效的抗惊厥药，可减少孕烷 X 受体的激活。它对 Cav3.1 (a1G) 和 Cav3.2 (a1H) 通道在 -80 mV 和- 100 mV 保持电位上具有同样的作用，IC50 值分别为 89 和 92 nM。它可用于多种人类神经系统疾病的研究，包括睡眠障碍和癫痫。
T30892	Chlordene AI3-15150,AI3 15150,AI315150
	Chlordene, as a polychlorinated flame retardant, has bioaccumulation and biomagnification potentials.
TP1531	Guangxitoxin 1E
	Guangxitoxin 1E acts as a gating modifier since it shifts the voltage-dependence of Kv2.1 K+ currents towards depolarized potentials.
T29748	AHR-12234
	AHR-12234 affects cardiac action potentials.
T26092	Risotilide
	Risotilide is a voltage-dependent potassium channel inhibitor. It can prolong cardiac action potentials and refractory periods.
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.
T4550L	Ajmaline hydrochloride
	Ajmaline hydrochloride is an alkaloid found in the root of Rauwolfia serpentina, and other plant sources. It is a class of Ia antiarrhythmic agent that apparently works by changing the shape and threshold of cardiac action potentials.
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。
T75360	Oxonol VI
	Oxonol VI 是一种膜电位的光学指示剂，在脂质囊泡中发挥作用。它能用于监测重组囊泡中与 (Na++K+)-ATPase 活性相关的膜电位变化。
T82057	Iota-conotoxin RXIA
	Iota-conotoxin RXIA是一种作用于电压门控钠通道（Nav1.2, 1.6, 1.7）的激动剂，其在小鼠脑内注射后能够引发青蛙运动神经轴突的重复动作电位以及癫痫样发作。
T80168	Scorpion toxin Tf2	Sodium Channel	Membrane transporter/Ion channel
	Scorpion toxin Tf2为一种在Tityus fasciolatus的毒液中首次发现的β-蝎毒素。作为Nav1.3激活剂，该毒素与神经元的电压门控钠（Nav）亚型相关，此亚型与癫痫和伤害感受密切相关。Scorpion toxin Tf2作用于hNav1.3，能够增强其激活电压，并且能够在静息膜电位下开启该通道。
T62942	Moricizine Hydrochloride
	Moricizine Hydrochloride (EN 313) 是一种口服具有活力的 I 类抗心律失常剂。Moricizine Hydrochloride 能够减少 0 相去极化的速率；提高 2 相和 3 相复极率，降低动作电位持续时间，减少有效不应期。
T62822	CT1-3
	CT1-3 是一种有效的抗癌剂。CT1-3 能够调控 JNK/Bcl-2/Bax/XIAP 通路，进而诱导线粒体介导的细胞凋亡 (apoptosis)。CT1-3 可以调控 E-cadherin/Snail 轴抑制人癌细胞 (HCCs) 的上皮间充质转化 (EMT) 电位，并抑制肿瘤发生。CT1-3 在小鼠模型中具有抗肿瘤作用，且没有表现出明显的肝、肾毒性。
T78060	ProTx II TFA	Sodium Channel	Membrane transporter/Ion channel
	ProTx-II TFA是选择性作用于Nav1.7钠通道的阻滞剂，具有0.3 nM的IC50值，选择性比其他钠通道亚型高出至少100倍。该化合物抑制钠离子通道，通过减少通道电导及使激活电压向更正的电位移动，从而阻断痛觉感受器中动作电位的传导。
T37215	5α,6β-Dihydroxycholestanol
	5α,6β-Dihydroxycholestanol is an oxysterol metabolite of cholesterol formed from conversion of cholesterol epoxides by 5,6-epoxysterol hydrolase. It inhibits NMDA-mediated calcium influx in HEK293 cells expressing NR1/NR2B NMDA receptors in a concentration-dependent manner. It also binds to voltage-gated sodium (Nav) channels and decreases action potentials in hippocampal neurons in vitro when used at a concentration of 10 uM. It increases survival of spinal cord motoneurons, cortical neurons, a...
T79718	CaMKIIα-PHOTAC	CaMK	Neuroscience
	CaMKIIα-PHOTAC是一种靶向Ca2+/钙调蛋白依赖性蛋白激酶IIα（CaMKIIα）的光化学靶向嵌合体（PHOTAC）。该分子在特定波长光照射下实现靶蛋白的泛素化及通过蛋白酶体催化的降解。CaMKIIα-PHOTAC能在光照条件下显著降低小鼠海马区域的诱发LTP反应强度，减弱突触功能，并对维护亚细胞级别的树突结构域、长时程增强及记忆能力起到关键作用。
T83732	Tat-CBD3A6K TFA
	Tat-CBD3A6K是一种肽类化合物，为N型电压门控钙通道Cav2.2以及collapsin response mediator protein 2 (CRMP2) 蛋白-蛋白相互作用抑制剂Tat-CBD3的衍生物。Tat-CBD3A6K (10 mg/kg) 能够阻止由d4T (stavudine)引发的大鼠抗逆转录病毒神经病痛模型中爪撤回阈值的下降，并减少同一大鼠分离的背根神经节(DRG)神经元的动作电位数量。通过硬膜途径给予Tat-CBD3A6K (30 µM/animal) 能够减少由萜类生物碱辣椒素引发的大鼠硬脑膜血流增加。
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

Cat.No: T22514

Target: 5-HT Receptor

Cat.No: T3478

Target: GluR

Cat.No: T17197

Cat.No: T38192

Target: Others

Cat.No: T4440

Target: GABA Receptor

Cat.No: T8944

Target: Calcium Channel

Cat.No: T30892

Synonym: AI3-15150,AI3 15150,AI315150

Guangxitoxin 1E

Cat.No: TP1531

Cat.No: T29748

Cat.No: T26092

Asocainol hydrochloride

Cat.No: T68361

Ajmaline hydrochloride

Cat.No: T4550L

Cat.No: T68918

Heteropodatoxin-2

Cat.No: T80434

Target: Potassium Channel

Cat.No: T75360

Iota-conotoxin RXIA

Cat.No: T82057

Scorpion toxin Tf2

Cat.No: T80168

Target: Sodium Channel

Moricizine Hydrochloride

Cat.No: T62942

Cat.No: T62822

Cat.No: T78060

Target: Sodium Channel

5α,6β-Dihydroxycholestanol

Cat.No: T37215

CaMKIIα-PHOTAC

Cat.No: T79718

Target: CaMK

Tat-CBD3A6K TFA

Cat.No: T83732

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Cat. No.	Product Name	Target	Signaling Pathways
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。
TN1727	Helichrysetin 4,2',4'-三羟基-6'-甲氧基查耳酮,蜡菊亭	Apoptosis; HIV Protease	Apoptosis; Microbiology/Virology; Proteases/Proteasome
	Helichrysetin 是从豆蔻果实中分离出的一种天然产物，是一种 DNA 结合抑制剂，可抑制原位导管癌DCIS 的形成。它抑制细胞生长，可诱导 A549 细胞凋亡。
T36068	Brevetoxin B
	Brevetoxin B is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. It binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50 = 15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning.
TN5463	Leachianone G
	Leachianone G exhibits significant antioxidant potentials in the ABTS, ONOO(-), and total ROS assays, it also shows inhibitory activities against pancreatic lipase, it may be used as drug candidate to control obesity. Leachianone G shows potent antiviral
T81957	Lacto-N-triose II
	Lacto-N-triose II 作为人乳低聚糖(HMOs)的核心结构单位，具备用于合成复杂HMOs的营养潜力。
TN6570	Daturaolone
	Daturaolone has potency in reducing the harmful effects or in maintaining the normal hepatic physiological mechanisms in both acute and chronic hepato-toxic induced liver damage in rats. Daturaolone also possesses in vivo anti-inflammatory and antinocicep
T4960	VASICINE	Anti-infection; AChR	Microbiology/Virology; Neuroscience
	Vasicine 是一种分离自Justicia adhatoda 中的喹唑啉类生物碱。它具有抗结核作用。
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。
TN4223	Homopterocarpin	Antifection	Microbiology/Virology
	Homopterocarpin and Pterocarpus extract offer gastroprotection against indomethacin- induced ulcer by antioxidative mechanism and the modulation of gastric homeostasis, homopterocarpin may be responsible for, or contribute to the antiulcerogenic property

天然产物

Cat.No: T8195

Target: Others

Cat.No: TN1727

Synonym: 4,2',4'-三羟基-6'-甲氧基查耳酮,蜡菊亭

Target: Apoptosis, HIV Protease

Cat.No: T36068

Cat.No: TN5463

Lacto-N-triose II

Cat.No: T81957

Cat.No: TN6570

Cat.No: T4960

Target: Anti-infection, AChR

Lotusine hydroxide

Cat.No: T78489

Homopterocarpin

Cat.No: TN4223

Target: Antifection

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