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ICA-121431 {[allProObj[0].p_purity_real_show]}

货号:A181030 Ambeed 开学季,买赠积分,赢豪礼

ICA-121431 是一种纳摩尔级别强效广谱电压门控钠通道 (Nav) 阻滞剂,对人 Nav1.1 和 Nav1.3 亚型具有等效选择性,IC50s 小于20 nM,ICA-121431 对人Nav1.2 的抑制作用较弱 (IC50=240 nM),而对人Nav1.4、Nav1.5、Nav1.6、Nav1.7和Nav1.8通道表现出大于 1000 倍的选择性(IC50s >10 µM)。ICA-121431可以抑制大鼠的Nav1.7通道(IC50=19nM)。

ICA-121431 化学结构 CAS号:313254-51-2
ICA-121431 化学结构
CAS号:313254-51-2
ICA-121431 3D分子结构
CAS号:313254-51-2
ICA-121431 化学结构 CAS号:313254-51-2
ICA-121431 3D分子结构 CAS号:313254-51-2
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ICA-121431 纯度/质量文件 产品仅供科研

货号:A181030 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Sodium Channel 其他靶点 纯度
Tolperisone HCl {[allProObj[0].p_purity_real_show]}
Lamotrigine {[allProObj[0].p_purity_real_show]}
Vinpocetine {[allProObj[0].p_purity_real_show]}
Zonisamide {[allProObj[0].p_purity_real_show]}
Dronedarone Hydrochloride {[allProObj[0].p_purity_real_show]}
Procainamide hydrochloride {[allProObj[0].p_purity_real_show]}
Bupivacaine HCl {[allProObj[0].p_purity_real_show]}
Benzocaine {[allProObj[0].p_purity_real_show]}
Carbamazepine ++

Sodium channel, IC50: 131 μM

{[allProObj[0].p_purity_real_show]}
Ibutilide fumarate {[allProObj[0].p_purity_real_show]}
Dibucaine HCl {[allProObj[0].p_purity_real_show]}
Mexiletine HCl {[allProObj[0].p_purity_real_show]}
Phenytoin {[allProObj[0].p_purity_real_show]}
Camostat Mesylate +++

epithelial sodium channel (ENaC), IC50: 50 nM

{[allProObj[0].p_purity_real_show]}
Levobupivacaine {[allProObj[0].p_purity_real_show]}
Oxcarbazepine +

sodium channel, IC50: 160 μM

{[allProObj[0].p_purity_real_show]}
Ambroxol {[allProObj[0].p_purity_real_show]}
Primidone {[allProObj[0].p_purity_real_show]}
Propafenone {[allProObj[0].p_purity_real_show]}
A-803467 ++++

Na(V1.8) channel, IC50: 8 nM

{[allProObj[0].p_purity_real_show]}
Rufinamide {[allProObj[0].p_purity_real_show]}
Phenytoin sodium {[allProObj[0].p_purity_real_show]}
Proparacaine Hydrochloride +

Voltage-gated sodium channel, ED50: 3.4 mM

{[allProObj[0].p_purity_real_show]}
Riluzole {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

ICA-121431 生物活性

描述 ICA-121431 is a nanomolar potent, broad-spectrum blocker of voltage-gated sodium channels (Nav), exhibiting particularly strong selectivity for the human Nav1.1 and Nav1.3 subtypes, with IC50 values of 13 nM and 23 nM, respectively[1]. For wild type human Nav channels, it shows IC50 values of 0.013 µM for hNav1.3, over 30 µM for hNav1.5, and 12 µM for hNav1.7, demonstrating its selective blocking capability[1]. ICA-121431 is against hNav channels with point mutations,showshNav1.3/hNav1.5 S1-S4, hNav1.3/hNav1.5 S3-S4, hNav1.3/hNav1.5 S5-S6, hNav1.3/hNav1.7 S1, hNav1.3/hNav1.7 S2, hNav1.3/hNav1.7 S3-S4, and hNav1.3/hNav1.7 S5-S6 with IC50 values of 0.083 µM, 1.2 µM, 11 µM, 2.0 µM, 0.045 µM, 0.030 µM, 0.30 µM, 1.0 µM, and 0.024 µM, respectively[1].
体外研究

ICA-121431 is a nanomolar potent, broad-spectrum blocker of voltage-gated sodium channels (Nav), exhibiting particularly strong selectivity for the human Nav1.1 and Nav1.3 subtypes, with IC50 values of 13 nM and 23 nM, respectively[1].

For wild type human Nav channels, it shows IC50 values of 0.013 µM for hNav1.3, over 30 µM for hNav1.5, and 12 µM for hNav1.7, demonstrating its selective blocking capability[1].

ICA-121431 is against hNav channels with point mutations,showshNav1.3/hNav1.5 S1-S4, hNav1.3/hNav1.5 S3-S4, hNav1.3/hNav1.5 S5-S6, hNav1.3/hNav1.7 S1, hNav1.3/hNav1.7 S2, hNav1.3/hNav1.7 S3-S4, and hNav1.3/hNav1.7 S5-S6 with IC50 values of 0.083 µM, 1.2 µM, 11 µM, 2.0 µM, 0.045 µM, 0.030 µM, 0.30 µM, 1.0 µM, and 0.024 µM, respectively[1].

ICA-121431 参考文献

[1]McCormack K, et al. Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels.Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):E2724-32.

ICA-121431 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.12mL

2.22mL

1.11mL

22.24mL

4.45mL

2.22mL

ICA-121431 技术信息

CAS号313254-51-2
分子式C23H19N3O3S2
分子量 449.545
别名
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 45 mg/mL(100.1 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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