ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.
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产品名称 | Sodium Channel ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tolperisone HCl | ✔ | 99% | |||||||||||||||||
Lamotrigine | ✔ | 98% | |||||||||||||||||
Vinpocetine | ✔ | 98% | |||||||||||||||||
Zonisamide | ✔ | 99% | |||||||||||||||||
Dronedarone HCl | ✔ | 95% | |||||||||||||||||
Procainamide HCl | ✔ | 99% | |||||||||||||||||
Bupivacaine HCl | ✔ | 99+% | |||||||||||||||||
Benzocaine | ✔ | 98% | |||||||||||||||||
Carbamazepine |
++
Sodium channel, IC50: 131 μM |
98% | |||||||||||||||||
Quinidine sulfate dihydrate | ✔ | 98% | |||||||||||||||||
Ibutilide fumarate | ✔ | 99%+ | |||||||||||||||||
Dibucaine HCl | ✔ | 99+% | |||||||||||||||||
Mexiletine HCl | ✔ | 99% | |||||||||||||||||
Phenytoin | ✔ | 99+% | |||||||||||||||||
Camostat Mesylate |
+++
epithelial sodium channel (ENaC), IC50: 50 nM |
99%+ | |||||||||||||||||
Levobupivacaine | ✔ | 97+% | |||||||||||||||||
Oxcarbazepine |
+
sodium channel, IC50: 160 μM |
98% | |||||||||||||||||
Ambroxol | 98+% | ||||||||||||||||||
Primidone | ✔ | 99% | |||||||||||||||||
Propafenone | ✔ | 99% | |||||||||||||||||
A-803467 |
++++
Na(V1.8) channel, IC50: 8 nM |
99%+ | |||||||||||||||||
Rufinamide | ✔ | 99% | |||||||||||||||||
Phenytoin sodium | ✔ | 98% | |||||||||||||||||
Proparacaine HCl |
+
Voltage-gated sodium channel, ED50: 3.4 mM |
98+% | |||||||||||||||||
Riluzole | ✔ | 97% | |||||||||||||||||
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。 |
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]. |
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 |
CAS号 | 313254-51-2 |
分子式 | C23H19N3O3S2 |
分子量 | 449.55 |
SMILES Code | O=C(NC1=CC=C(S(NC2=NC=CS2)(=O)=O)C=C1)C(C3=CC=CC=C3)C4=CC=CC=C4 |
MDL No. | MFCD00992334 |
别名 | |
运输 | 蓝冰 |
InChI Key | URSQNPPONHUJDL-UHFFFAOYSA-N |
Pubchem ID | 998021 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, store in freezer, under -20°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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