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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8579 |
Nav1.8-IN-1
5-(4-Chlorophenyl)-N-[[2-(2,2,2-trifluoroethoxy)pyridin-3-yl]methyl]pyridine-3-carboxamide,CHEMBL1270208 |
Sodium Channel | Membrane transporter/Ion channel |
Nav1.8-IN-1 (CHEMBL1270208) 是一种有效的 Na(v)1.8 钠通道抑制剂,可用于研究精神性疼痛及炎症性疼痛。 | |||
T77693 |
Nav1.8-IN-4
|
Sodium Channel | Membrane transporter/Ion channel |
Nav1.8-IN-4 是一种有效的 Nav1.8 通道抑制剂,具有潜在的镇痛活性。Nav1.8-IN-4 可用于疼痛和神经系统相关疾病。 | |||
T62422 |
Nav1.8-IN-2
|
Others | Others |
Nav1.8-IN-2 (compound 35A) 是一种 Nav1.8 的有效抑制剂 (IC50: 0.4 nM)。Nav1.8-IN-2 能够用于疼痛障碍、咳嗽、急性和慢性瘙痒症的研究。 | |||
T2024 |
A-803467
A 803467,A803467 |
Sodium Channel | Membrane transporter/Ion channel |
A-803467 是有效的、选择性的河豚毒素不敏感型Nav1.8 钠通道阻断剂 。它在炎症性疼痛和神经性疼痛模型中有缓解疼痛作用。它通过与 ATP-binding cassette subfamily G member 2 (ABCG2) 转运蛋白的相互作用,增强了传统抗癌物的化疗敏感性。 | |||
T12424 |
PF-06305591
PF-6305591 |
Others | Others |
PF-06305591是一种有效的、选择性的电压门钠通道NaV1.8的阻断剂(IC50=15 nM)。 | |||
T4490 |
PF-01247324
|
Sodium Channel | Membrane transporter/Ion channel |
PF01247324是一种选择性的、口服有效的Nav1.8通道阻断物,对人类重组Nav1.8 的IC50为196 nM。 | |||
T62000 |
ABBV-318
|
Others | Others |
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。 | |||
T84298 |
LTGO-33
|
Sodium Channel | Membrane transporter/Ion channel |
LTGO-33 是一种具有物种特异性的电压门控钠通道 NaV1.8 抑制剂,抑制 NaV1.8、 NaV1.1-NaV1.7 和 NaV1.9。LTGO-33 抑制野生型和多重 NaV1.8 与人类疼痛疾病相关的变异,可用于研究疼痛。 | |||
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。 | |||
T9683 |
VX-150
|
Sodium Channel | Membrane transporter/Ion channel |
VX-150 是一种口服有效的,高选择性的 NaV1.8抑制剂。VX-150 在各种疼痛适应症中有研究的价值。 | |||
T16514 |
PF 04531083
|
Others; Sodium Channel | Membrane transporter/Ion channel; Others |
PF 04531083 是 NaV1.8 通道的特异性阻断剂。 PF 04531083 可用于神经性和炎症性疼痛的相关研究。 | |||
T12421 |
PF-04885614
|
Sodium Channel | Membrane transporter/Ion channel |
PF-04885614是一种有效的NaV1.8抑制剂。PF-04885614有用于神经系统疾病和神经发育疾病研究的潜力。 | |||
T69552 |
Suzetrigine
VX-548 |
Sodium Channel | Membrane transporter/Ion channel |
Suzetrigine(VX-548) 是一种具有口服活性和特异性的 NaV1.8 抑制剂。 Suzetrigine 具有镇痛活性,可用于研究急性疼痛和神经通。 | |||
T37688 |
Cyfluthrin
|
Reactive Oxygen Species; Sodium Channel | Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; NF-κB |
Cyfluthrin 属于 II 型拟除虫菊酯,对多种昆虫都有杀灭效果。Cyfluthrin 是Nav1.8钠通道调节剂。它可应用于农业、兽医、杀虫剂、拟除虫菊酯和贮存产品等领域。 | |||
T69915 |
GX-585
GX585,GX 585 |
Sodium Channel | Membrane transporter/Ion channel |
GX-585 是一种磺胺类化合物,是一种Nav 1.7通道抑制剂,具有镇痛活性,可用于研究神经疼痛和炎症。 | |||
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。 | |||
T23136 |
PF 04885614
|
Others | Others |
NaV1.8 inhibitor | |||
T78955 |
Analgesic agent-2
|
Sodium Channel | Membrane transporter/Ion channel |
Analgesic agent-2为一选择性且活性的NaV1.8 Channel抑制剂,其IC50为50.18 nM,作用于稳定表达人NaV1.8的HEK293细胞,具有镇痛活性。 | |||
T60761 |
PF-06305591 dihydrate
|
Others | Others |
PF-06305591 dihydrate 是具有出色的临床前体外 ADME 和安全性的,电压门控钠通道 NaV1.8的高选择性阻断剂 (IC50 = 15 nM)。 | |||
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。 | |||
TP1968 |
ProTx-I
ProTx I |
||
Selective CaV3.1 channel blocker (IC50 values are 0.2 and 31.8 μM for hCaV3.1 and hCaV3.2 respectively). Also reversibly inhibits NaV1.8 and blocks KV2.1 channels. | |||
TP2081 |
APETx2
|
||
Acid-sensing ion channel 3 (ASIC3) channel blocker (IC50 values are 63 and 175 nM for homomeric rat and human ASIC3 channels). Also inhibits NaV1.8 and NaV1.2 channels (IC50 values are 55 and 114 nM respectively). Demonstrates analgesic properties against | |||
T80452 |
Ceratotoxin-1
CcoTx1,β-TRTX-cm1a |
Sodium Channel | Membrane transporter/Ion channel |
Ceratotoxin-1 (CcoTx1)为电压门控钠通道亚型的抑制剂,特别是对Nav1.1/β1、Nav1.2/β1、Nav1.4/β1和Nav1.5/β1具有不同程度的抑制效果,其IC50值分别为523 nM、3 nM、888 nM和323 nM。此外,Ceratotoxin-1对Nav1.8/β1亦有抑制作用。 | |||
T37093 |
4,9-Anhydrotetrodotoxin
4,9-Anhydrotetrodotoxin,4,9-anhydro-TTX |
Others | Others |
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 µM for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1] | |||
TP2003 |
Mambalgin 1
|
||
Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases late | |||
T80851 |
VSTx-3
Kappa-TRTX-Gr4a,κ-Theraphotoxin-Gr4a,Voltage sensor toxin 3,Peptide F |
||
VSTx-3是KV通道阻断剂,同时也是TTX敏感钠通道尤其是NaV1.8通道的有效阻断剂。具体而言,其对hNaV1.3通道的IC50为0.19 μM,对hNaV1.7通道的IC50为0.43 μM,对hNaV1.8通道的IC50为0.77 μM。 | |||
T75954 |
Mambalgin 1 TFA
|
||
Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests. | |||
T75594 |
Harpactira Baviana Venom
|
Others | Others |
Harpactira Baviana Venom (Baboon Tarantula Venom) 是一种蜘蛛毒液,能够从皇帝巴布蜘蛛蜘蛛中获得。Harpactira Baviana Venom 可以调节 NaV1.8和诱导痛觉过敏。 | |||
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。 | |||
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. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 |