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15

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
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。
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。
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。
T37093 4,9-Anhydrotetrodotoxin

4,9-Anhydrotetrodotoxin,4,9-anhydro-TTX

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 &#181M for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1]
T80425 Jingzhaotoxin-V

Sodium Channel Membrane transporter/Ion channel
Jingzhaotoxin-V是Chilobrachys jingzhao蜘蛛毒液中的一种含29个氨基酸残基的多肽。该化合物抑制大鼠背根神经节神经元的河豚毒素抗性和河豚毒素敏感sodium currents,相应IC50值为27.6 nM与30.2 nM。同时,Jingzhaotoxin-V也能抑制表达在爪蟾卵母细胞中的Kv4.2钾电流,IC50值为604.2 nM。
T28227 Oe-9000

Oe 9000

Oe-9000 is a blocker of voltage-gated Na(+) currents in neurons. It reversibly reduces rapidly activating and inactivating TTX-sensitive (TTX-S) Na(+) currents as well as slowly activating and inactivating tetrodotoxin-resistant (TTX-R) Na(+) currents at
T80428 Jingzhaotoxin-34

Sodium Channel Membrane transporter/Ion channel
Jingzhaotoxin-34是一种含35个氨基酸残基的多肽神经毒素,能特异性抑制TTX-S钠电流(IC50约85 nM),对大鼠背根神经节TTX-R钠电流无显著作用。
T80426 Jingzhaotoxin-IX

Sodium Channel Membrane transporter/Ion channel
Jingzhaotoxin-IX是由35个氨基酸残基组成的C端酰胺化神经毒素。该化合物既抑制电压门控钠通道(包括河豚毒素抗性和河豚毒素敏感亚型)又抑制Kv2.1通道,但对延迟整流钾通道Kv1.1、1.2和1.3无效。
T80186 Hainantoxin-III

Sodium Channel Membrane transporter/Ion channel
Jingzhaotoxin-V是一种多肽,具有抑制作用,IC50值为604.2 nM,可显著抑制非洲爪蟾卵母细胞的钾电流。此外,Jingzhaotoxin-V对大鼠背根神经节神经元中的河豚毒素抗性钠电流和河豚毒素敏感钠电流也有抑制效果,其IC50值分别为27.6 nM和30.2 nM[1]。
T71122 Carsatrin (free base)

Carsatrin is purinylpiperazine derivative. as cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+, K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin
T80488 µ-Conotoxin SIIIA

Sodium Channel Membrane transporter/Ion channel
μ-Conotoxin SIIIA为TTX抗性sodium channel拮抗剂,属于毒性肽类,源自Conus snails毒液。该化合物主要应用于神经系统疾病,尤指神经性疼痛的研究。
T70975 Carsatrin succinate

Carsatrin succinate is the salt form of Carsatin, a purinylpiperazine derivative used as a cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+, K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbi...
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。
T80189 Hainantoxin-IV

HNTX-IV

Sodium Channel Membrane transporter/Ion channel
Hainantoxin-IV是针对河豚毒素敏感(TTX-S)电压门控钠通道的特异性拮抗剂。该化合物以His28和Lys32为主要残基与靶标结合,并采用了抑制剂胱氨酸结基序。
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。

化合物

PF 05089771 tosylate
Cat.No: T7502
Synonym:
Target: Sodium Channel
PF 05089771
Cat.No: T7502L
Synonym: PF-05089771,PF05089771
Target: Sodium Channel
A-803467
Cat.No: T2024
Synonym: A 803467,A803467
Target: Sodium Channel
4,9-Anhydrotetrodotoxin
Cat.No: T37093
Synonym: 4,9-Anhydrotetrodotoxin,4,9-anhydro-TTX
Target:
Jingzhaotoxin-V
Cat.No: T80425
Synonym:
Target: Sodium Channel
Oe-9000
Cat.No: T28227
Synonym: Oe 9000
Target:
Jingzhaotoxin-34
Cat.No: T80428
Synonym:
Target: Sodium Channel
Jingzhaotoxin-IX
Cat.No: T80426
Synonym:
Target: Sodium Channel
Hainantoxin-III
Cat.No: T80186
Synonym:
Target: Sodium Channel
Carsatrin (free base)
Cat.No: T71122
Synonym:
Target:
µ-Conotoxin SIIIA
Cat.No: T80488
Synonym:
Target: Sodium Channel
Carsatrin succinate
Cat.No: T70975
Synonym:
Target:
VSTx-3
Cat.No: T80851
Synonym: Kappa-TRTX-Gr4a,κ-Theraphotoxin-Gr4a,Voltage sensor toxin 3,Peptide F
Target:
Hainantoxin-IV
Cat.No: T80189
Synonym: HNTX-IV
Target: Sodium Channel
mHuwentoxin-IV
Cat.No: T80495
Synonym:
Target: Sodium Channel
Cat. No. Product Name Target Signaling Pathways
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。
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。

天然产物

3-Deoxyaconitine
Cat.No: T4S1876
Synonym:
Target: Sodium Channel
Hardwickiic acid
Cat.No: TN4183
Synonym: (-)-Hardwikiic acid
Target: Sodium Channel
TargetMol Loading
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