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64

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12181	NaV1.7 inhibitor-1	Sodium Channel	Membrane transporter/Ion channel
	NaV1.7 inhibitor-1 是有效的、选择性的电压门控钠通道 (Nav) 1.7 抑制剂，对于hNaV1.7的IC50为 0.6 nM，其选择性是 hNaV1.5 的 80 倍。
T38911	Nav1.7-IN-8 Nav1.7-IN-8
	Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP2C9 and CYP3A4, with IC50 values of 0.17 μM and 0.077 μM, respectively. Notably, Nav1.7-IN-8 demonstrates significant analgesic properties in rodent models of both acute and inflammatory pain.
T12184	Nav1.7 inhibitor	Others	Others
	Nav1.7 inhibitor is a potent inhibitor of Nav1.7.
T28132	NaV1.7 Blocker-801
	NaV1.7 Blocker-801 is a potent NaV1.7 blocker.
T12180	Nav1.7-IN-6	Others	Others
	Nav1.7-IN-6, a selective inhibitor of Nav1.7.
T12183	Nav1.7-IN-3	Others	Others
	Nav1.7-IN-3 is a selective and orally bioavailable inhibitor of voltage-gated sodium channel Nav1.7(IC50 of 8 nM).
T12182	Nav1.7-IN-2	Others	Others
	Nav1.7-IN-2 is avoltage-gated sodium channels (Nav) inhibitor in particular Nav 1.7(IC50 of 80 nM).
T8711	PF-05186462 PF-05150122	Sodium Channel	Membrane transporter/Ion channel
	PF-05186462 (PF-05150122)是选择性的人Nav1.7电压依赖性钠通道抑制剂，IC50为 21 nM，与其他钠通道 (Nav 1.1、1.2、1.3、1.4、1.5、1.6 和 1.8) 相比，它对 Nav1.7显示出显著的选择性。PF-05186462在急性或慢性疼痛中具有研究价值。
T7336	ICA-121431 2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl	Sodium Channel	Membrane transporter/Ion channel
	ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) 是强效的、广谱的电压门控钠通道阻滞剂，对人 Nav1.1 和 Nav1.3 亚型具有等效选择性，IC50分别为 13 nM 和 23 nM。它对Nav1.2 的抑制作用较弱，IC50为240 nM，对 Nav1.4、Nav1.6、抗TTX 的人 Nav1.5、Nav1.8 通道表现出大于 1000 倍的选择性，IC50>10 μM。
T12655	(Rac)-AMG8379 (Rac)-AMG8380	Sodium Channel	Membrane transporter/Ion channel
	(Rac)-AMG8379 ((Rac)-AMG8380) 是 AMG8379 的外消旋体，是一种具有口服活性和选择性的磺胺 NaV1.7 拮抗剂。
TQ0014	GNE-131	Sodium Channel	Membrane transporter/Ion channel
	GNE-131 是有效的人类钠离子通道 NaV1.7(hNaV1.7)选择性抑制剂，IC50为 3 nM。
T7502	PF 05089771 tosylate	Sodium Channel	Membrane transporter/Ion channel
	PF 05089771 tosylate 是口服有效的、选择性的Nav1.7丙烯酰胺抑制剂。PF 05089771 tosylate 具有用于疼痛和糖尿病神经性疾病的研究。
T9685	DS-1971a	Sodium Channel	Membrane transporter/Ion channel
	DS-1971a 是选择性、口服有效的 NaV1.7抑制剂，对 hNaV1.7 和 mNaV1.7 的 IC50分别为 22.8 和 59.4 nM。DS-1971a 在缓解疼痛方面有研究价值。
T23439	TC-N 1752	Sodium Channel	Membrane transporter/Ion channel
	TC-N 1752 是一种具有口服活性的 Nav1.7 通道抑制剂，IC50 为 0.17 μM。 TC-N 1752 显示镇痛活性。
T17263	XEN907	Others	Others
	XEN907 is a novel spiro oxindole NaV1.7 blocker. XEN907 also inhibits hNaV1.7 (IC50: 3 nM).
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。
T62000	ABBV-318
	ABBV-318可被当作治疗疼痛的小分子Nav1.7/ Nav1.8阻滞剂，对hNav1.7 和 hNav1.8具有抑制作用， IC50 值分别为 2.8 μM 和 3.8 μM。ABBV-318 可以用于研究与疼痛相关的疾病。
T9461	AZ194	Sodium Channel	Membrane transporter/Ion channel
	CRMP2-Ubc9-NaV1.7 inhibitor 194 是一流的CRMP2-Ubc9相互作用抑制剂及NaV1.7抑制剂 (IC50=1.2 μM)，口服有活性，具有抗伤害作用。AZ194 阻断 CRMP2 的 SUMOylation 以选择性地减少表面表达 NaV1.7 的量。
T50030	1-(2,4-difluorophenyl)guanidine hydrochloride	Others	Others
	1-(2,4-difluorophenyl)guanidine hydrochloride 是一种化合物，是电压门控钠通道Nav1.7的强效选择性抑制剂，Nav1.7是疼痛信号传输的关键参与者，因此它能够减少疼痛信号的传递，从而产生镇痛作用。
T9647	GX 201 GX-201	Sodium Channel	Membrane transporter/Ion channel
	GX 201 是选择性的 NaV1.7 抑制剂，其对 hNaV1.7 的 IC50 值为 <3.2 nM。
T15174	DSP-2230	Sodium Channel	Membrane transporter/Ion channel
	DSP-2230 是有效的Nav1.7/Nav1.8通道选择性阻断剂。
T15358	Funapide TV 45070,XEN402	Sodium Channel	Membrane transporter/Ion channel
	Funapide (TV 45070) 是一个有效的钠通 Nav1.7 抑制剂，据有潜在的抗炎活性，可用来治疗红斑性肢痛症、肌肉骨骼疼痛、膝关节炎以及疱疹后神经。
T34081	Piromelatine NEU-P-11,NEU-P 11,NEU-P11	P2X Receptor; 5-HT Receptor; MT Receptor; Sodium Channel; TRP/TRPV Channel	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Piromelatine 是褪黑激素 MT1/MT2 受体、5-HT1A 和 5-HT1D 的激动剂，也是 5-HT2B 的拮抗剂。Piromelatine 具有抗痛觉活性，对 P2X3、TRPV1 和 Nav1.7 通道有抑制作用，可用于促进睡眠、缓解疼痛、抗神经退行性疾病和抗抑郁疾病的研究。
T2342	Raxatrigine CNV1014802,CNV 1014802,GSK-1014802,CNV-1014802	Sodium Channel	Membrane transporter/Ion channel
	Raxatrigine (CNV 1014802) 是有效的钠离子通道 Nav1.7抑制剂。
T24520	NAV26 NAV-26,NAV 26
	NAV26 is a selective blocker of the Nav1.7 channel.
T16487	PF-05241328	Others	Others
	PF-05241328 is an effective and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (IC50: 31 nM).
T11439	GNE-616	Others	Others
	GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor (Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7) for the treatment of chronic pain.
T14201	AM-2099	Others	Others
	AM-2099 is a voltage-gated sodium channel Nav1.7 inhibitor (IC50: 0.16 μM).
T71166	PF-05150122
	PF-05150122 is a novel potent and selective human Nav1.7 blocker.
T11437	GNE-0439	Others	Others
	GNE-0439 is a novel Nav1.7-selective inhibitor (IC50: 0.34 uM) and inhibits Nav1.5 (IC50: 38.3 μM). GNE-0439 inhibits mutant N1742K channels (IC50: 0.37 uM) in membrane potential assays.
T27521	GX-936 GX 936,PF 05196233,PF05196233,GX936,PF-05196233
	GX-936, a Nav1.7 inhibitor, inhibits Nav1.7 through a voltage-sensor trapping mechanism, likely by stabilizing inactivated states of the channel.
T27520	GX-395 GX 395
	GX-395 is a novel Nav1.7 inhibitor.
T22829	GX-674	Sodium Channel	Membrane transporter/Ion channel
	GX-674 是一种具有高效和选择性的电压门控钠通道 1.7 (Nav1.7) 拮抗剂，在 -40 mV 时测得 IC50 值为 0.1 nM，可用于研究炎症和神经性疼痛。
T33943	PF-04856264 PF-4856264,PF4856264,PF 4856264
	PF-04856264 is a potent and selective human Nav1.7 voltage-gated sodium channel inhibitor (IC50 = 28 nM).
T16485	PF-05198007	Others	Others
	PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771. PF-05198007 is an effective and selective arylsulfonamide Nav1.7 inhibitor.
T14992	Raxatrigine hydrochloride GSK-1014802 hydrochloride,CNV1014802 (hydrochloride)	Others	Others
	Raxatrigine hydrochloride is a state-dependent sodium channel blocker and a Nav1.7 sodium channel inhibitor.
T80042	GpTx-1	Sodium Channel	Membrane transporter/Ion channel
	GpTx-1作为NaV1.7选择性抑制剂，具有高效性，其半抑制浓度(IC50)为10 nM。
T28371	PF-06456384 PF 6456384,PF06456384,PF6456384,PF 06456384,PF-6456384
	PF-06456384 is a highly potent and selective NaV1.7 inhibitor with IC50 value of 0.01 nM.
T11377	GDC-0276	Others	Others
	GDC-0276, a potent, selective, reversible, and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM, offers potential for pain treatment while overcoming limitations associated with current pain medications, including addiction and off-target side effects. It is well tolerated and demonstrates a favorable pharmacokinetic profile.
TP2070	BDS I
	Potent and reversible Kv3.4 potassium channel blocker (IC50 = 47 nM); also attenuates inactivation of sodium currents by acting on Nav1.7 and Nav1.3 channels. Enhances TTX-sensitive sodium currents in rat small dorsal root ganglion neurons. Neuroprotective.
T75250	(R)-Funapide
	(R)-Funapide ((R)-TV 45070)为Funapide中活性较低的R-对映异构体，是一种高效的Nav1.7钠通道阻滞剂，应用于疼痛研究。
T80444	Phlo1b μ-TrTx-Phlo1b	Sodium Channel	Membrane transporter/Ion channel
	Phlo1b（μ-TrTx-Phlo1b）为含35个氨基酸残基的肽毒素，特异性抑制Nav1.7通道。相较之下，其对Nav1.2与Nav1.5的抑制作用较弱。
T69915	GX-585
	GX-585 is a novel potent inhibitor of NaV1.7 and highly selective against NaV1.5, having limited selectivity against NaV1.1 and NaV1.2.
T80450	Pe1b μ-TrTx-Pe1b	Sodium Channel	Membrane transporter/Ion channel
	Pe1b (μ-TrTx-Pe1b) 作为选择性Nav1.7抑制剂，展现出IC50为167 nM的活性。
TP1680	ProTx II
	Selective NaV1.7 channel blocker. Shifts activation gating positively and decreases current magnitude. Displays 100-fold selectivity over other sodium channel subtypes.
T80435	Heteropodatoxin-1	Potassium Channel	Membrane transporter/Ion channel
	Heteropodatoxin-1 (HpTx1)为蜘蛛肽毒素，主要作用为Kv4.2电流的抑制剂，同时能够抑制Nav1.7和激活Nav1.9, 但对Nav1.8无影响。
T79398	Ancistrotecine B	Sodium Channel	Membrane transporter/Ion channel
	Ancistrotecine B（化合物2）为Nav1.7通道抑制剂（IC50：0.73 μM），能减轻小鼠炎症所致疼痛。
T69728	SUN49199
	SUN49199, also known as NaV1.7 Blocker-13, is a novel selective blocker of NaV1.7 with little affinity for NaV 1.2, 1.3, or 1.6, being more potent at human vs guinea pig NaV1.7. SUN49199 was reported in Journal of Pharmacology and Experimental Therapeutics (2017), 361(1), 172-180. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/na...
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
T75856	Huwentoxin-IV TFA
	Huwentoxin-IV TFA是一种具有高效性和选择性的钠通道阻滞剂，能够抑制Nav1.7、Nav1.2、Nav1.3和Nav1.4神经元，其IC50分别为26、150、338和400nM。通过优先结合于神经毒素受体位点4，Huwentoxin-IV TFA特异性地阻断周围神经的Nav1.7亚型。该化合物适用于炎症性及神经性疼痛动物模型的研究。

化合物

NaV1.7 inhibitor-1

Cat.No: T12181

Target: Sodium Channel

Cat.No: T38911

Synonym: Nav1.7-IN-8

Nav1.7 inhibitor

Cat.No: T12184

Target: Others

NaV1.7 Blocker-801

Cat.No: T28132

Cat.No: T12180

Target: Others

Cat.No: T12183

Target: Others

Cat.No: T12182

Target: Others

Cat.No: T8711

Synonym: PF-05150122

Target: Sodium Channel

Cat.No: T7336

Synonym: 2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl

Target: Sodium Channel

Cat.No: T12655

Synonym: (Rac)-AMG8380

Target: Sodium Channel

Cat.No: TQ0014

Target: Sodium Channel

PF 05089771 tosylate

Cat.No: T7502

Target: Sodium Channel

Cat.No: T9685

Target: Sodium Channel

Cat.No: T23439

Target: Sodium Channel

Cat.No: T17263

Target: Others

Cat.No: T7502L

Synonym: PF-05089771,PF05089771

Target: Sodium Channel

Cat.No: T62000

Cat.No: T9461

Target: Sodium Channel

1-(2,4-difluorophenyl)guanidine hydrochloride

Cat.No: T50030

Target: Others

Cat.No: T9647

Synonym: GX-201

Target: Sodium Channel

Cat.No: T15174

Target: Sodium Channel

Cat.No: T15358

Synonym: TV 45070,XEN402

Target: Sodium Channel

Cat.No: T34081

Synonym: NEU-P-11,NEU-P 11,NEU-P11

Target: P2X Receptor, 5-HT Receptor, MT Receptor, Sodium Channel, TRP/TRPV Channel

Cat.No: T2342

Synonym: CNV1014802,CNV 1014802,GSK-1014802,CNV-1014802

Target: Sodium Channel

Cat.No: T24520

Synonym: NAV-26,NAV 26

Cat.No: T16487

Target: Others

Cat.No: T11439

Target: Others

Cat.No: T14201

Target: Others

Cat.No: T71166

Cat.No: T11437

Target: Others

Cat.No: T27521

Synonym: GX 936,PF 05196233,PF05196233,GX936,PF-05196233

Cat.No: T27520

Synonym: GX 395

Cat.No: T22829

Target: Sodium Channel

Cat.No: T33943

Synonym: PF-4856264,PF4856264,PF 4856264

Cat.No: T16485

Target: Others

Raxatrigine hydrochloride

Cat.No: T14992

Synonym: GSK-1014802 hydrochloride,CNV1014802 (hydrochloride)

Target: Others

Cat.No: T80042

Target: Sodium Channel

Cat.No: T28371

Synonym: PF 6456384,PF06456384,PF6456384,PF 06456384,PF-6456384

Cat.No: T11377

Target: Others

Cat.No: TP2070

Cat.No: T75250

Cat.No: T80444

Synonym: μ-TrTx-Phlo1b

Target: Sodium Channel

Cat.No: T69915

Cat.No: T80450

Synonym: μ-TrTx-Pe1b

Target: Sodium Channel

Cat.No: TP1680

Heteropodatoxin-1

Cat.No: T80435

Target: Potassium Channel

Ancistrotecine B

Cat.No: T79398

Target: Sodium Channel

Cat.No: T69728

Cat.No: TP2016

Synonym: Huwentoxin IV

Huwentoxin-IV TFA

Cat.No: T75856

Cat. No.	Product Name	Target	Signaling Pathways
T2173	Veratridine	Sodium Channel	Membrane transporter/Ion channel
	Veratridine 是一种生物碱，来自百合科植物。Veratridine 是一种钠通道激动剂，对 Nav1.7 的峰值电流具有抑制作用，IC50为 18.39 µM。
TN1254	3'-Methoxydaidzein 3'-甲氧基大豆苷元	Sodium Channel	Membrane transporter/Ion channel
	3'-Methoxydaidzein 是一种异黄酮和 Sodium Channel 双重抑制剂。3'-Methoxydaidzein 对NaV1.7、NaV1.8 和 NaV1.3有抑制作用，IC50 分别为 181 nM、397 nM 和 505 nM。 3'-Methoxydaidzein 对胶原诱导的血小板聚集具有特异性，IC50值分别为12.3和61.5µM。。3'-Methoxydaidzein 通过抑制电压门控钠通道发挥镇痛作用。 3'-Methoxydaidzein 具有抗氧化活性和抗血小板聚集活性。
T82764	Cd1a β-TRTX-cd1a,β-Theraphotoxin-cd1a
	Cd1a是从非洲蜘蛛Ceratogyrus darlingi中提取的β-毒素，具有调节钙离子通道的功能。它能够抑制人类的钙离子通道(Cav2.2)(IC50 2.6 μM)以及小鼠的钠离子通道(Nav1.7)，有望用于开发治疗外周疼痛的药物。

天然产物

Cat.No: T2173

Target: Sodium Channel

3'-Methoxydaidzein

Cat.No: TN1254

Synonym: 3'-甲氧基大豆苷元

Target: Sodium Channel

Cat.No: T82764

Synonym: β-TRTX-cd1a,β-Theraphotoxin-cd1a

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