ICA-121431 产品活性：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，IC50 值分别为 13 nM 和 23 nM。ICA-121431 对Nav1.2 的抑制作用较弱 (IC50=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(IC50s >10 µM)。 产品来源： https://www.medchemexpress.cn/ICA-121431.html 研究领域：Membrane Transporter/Ion Channel 作用靶点：Sodium Channel In Vitro: ICA-121431 interacts with human Nav1.3 and the amino acid residues that may define selectivity for this channel over other related Nav channels, including Nav1.7 and Nav 1.5. Data generated using conventional patch clamp electrophysiological recording using a pulse protocol whereby a 20-ms test pulse is preceded by an 8-s step to a voltage that inactivated half of the channels. ICA-121431 is against Wild type hNav1.3 hNav1.5 hNav1.7 with IC50s of 0.013 µM, >30 µM, 12 µM, respectively. ICA-121431 is against hNav channels with point mutations,shows hNav1.3 M1 (S1510Y), hNav1.3 M2 (R1511W), hNav1.3 M3 (E1559D), hNav1.3 M1,3 (S1510Y/E1559D), hNav1.3 M2, 3 (R1511W/E1559D), hNav1.3 M1, 2, 3 (S1510Y/R1511W/E1559D), and hNav1.7 M1, 2, 3 (Y1537S/W1538R/D1586E) with IC50 values of 0.1 µM, 0.37 µM, 1.1 µM, 1.3 µM, 1.9 µM, 11.6 µM, 0.032 µM, respectively. ICA-121431 is against hNav channels with point mutations,shows hNav1.3/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. 相关产品：Bioactive Compound Library Plus | Membrane Transporter/Ion Channel Compound Library | Peptidomimetic Library | Anti-Cardiovascular Disease Compound Library | Neuroprotective Compound Library | Mechanoreceptors Compound Library | Targeted Diversity Library | Sodium Channel Blocker Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Ion Channel Compound Library | Anti-Drug-Resistant Compound Library | Multi-Target Compound Library | Bioactive Compound Library Max | Amiloride hydrochloride | Halofuginone | Carbamazepine | Riluzole | 20(S)-Ginsenoside Rg3 | Lidocaine | TPC2-A1-P | Veratridine | Fluphenazine dihydrochloride | Amitriptyline hydrochloride | Lamotrigine | A-803467 | QX-314 chloride | 5-(N,N-Hexamethylene)-amiloride | Phenytoin | Triamterene | Ranolazine | Flunarizine dihydrochloride | Benzamil hydrochloride | Suzetrigine | Atomoxetine hydrochloride | Vinpocetine | Zandatrigine | Ropivacaine | PF 05089771 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。