MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 298684-44-3
MCE 国际站:ML402
产品活性:ML402,一种噻吩甲酰胺,是一种选择性的 K2P2.1 (TREK-1) 和 K2P10.1 (TREK-2) 活化剂,对 K2P4.1 (TRAAK) 无明显作用。
研究领域:Membrane Transporter/Ion Channel
作用靶点:Potassium Channel
In Vitro: Xenopus oocyte two-electrode voltage-clamp measurements show that ML335 and ML402 activate K2P2.1 and K2P10.1 but not K2P4.1(14.3±2.7 μM, K2P2.1-ML335; 13.7±7.0 μM, K2P2.1-ML402; 5.2±0.5 μM, K2P10.1-ML335; and 5.9±1.6 μM, K2P10.1-ML402). The K2P modulator pocket has a single difference among TREK subfamily members at the cation-π interaction position, K2P2.1 Lys271, which is also a lysine in K2P10.1 but a glutamine in K2P4.1.Swapping the Lys271 equivalent between K2P2.1 and K2P4.1 results in a clear phenotype reversal for ML335 and M402 activation. K2P2.1 (K271Q) is insensitive to ML335 and ML402, whereas K2P4.1 (Q258K) responds to both with a similar EC50 to K2P2.1 (14.3±2.7 μM, K2P2.1-ML335; 16.2±3.0 μM, K2P4.1(Q258K)-ML335; 13.7±7.0 μM, K2P2.1-ML402; 13.6±1.5 μM, K2P4.1 (Q258K)-ML402) but with a lower magnitude response than K2P2.1.
相关产品:Bioactive Compound Library Plus | Membrane Transporter/Ion Channel Compound Library | Neuroprotective Compound Library | Mechanoreceptors Compound Library | Targeted Diversity Library | Potassium Channel Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | Mitiglinide-d5 calcium | Ropivacaine hydrochloride | WX-081 | Doxapram hydrochloride hydrate | TASK-1-IN-1 | VU0134992 | BL-1249 | Dendrotoxin K | Disopyramide | Domiphen bromide | Dehydrosoyasaponin I | 20(S)-Ginsenoside Rg3 | (Rac)-Ropivacaine-d7 | AZD-5672 | Daurisoline | (+)-KCC2 blocker 1 | ML252 | Ketanserin | Ropivacaine mesylate | AMP-PNP tetralithium | PK-THPP | Ifenprodil tartrate | DDO-02005 | Hydrochlorothiazide-13C6 | Brompheniramine maleate | Meclofenamic acid sodium hydrate | DMP-543 | BAPTA-AM | PNU 37883 hydrochloride | Quinine hydrochloride dihydrate
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-104027
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 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;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 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。