Mirogabalin besylate 产品活性：Mirogabalin besylate 是一种选择性的，可口服的电压门控性钙通道 (voltage-gated calcium channels) 亚基 α2δ 的有效配体，对人 α2δ-1 和 α2δ-2，大鼠 α2δ-1 和 α2δ-2 的 Kd 值分别为 13.5 nM，22.7 nM，27 nM 和 47.6 nM。 产品来源： https://www.medchemexpress.cn/Mirogabalin_besylate.html 研究领域：Membrane Transporter/Ion Channel | Neuronal Signaling 作用靶点：Calcium Channel In Vitro: Mirogabalin besylate is a ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively. Mirogabalin shows binding affinity for the gabapentin binding site in rat cortical brain homogenates with the IC50 value of 16.0 nM. Mirogabalin has no effect on any other receptors, channels, transporters, or enzymes at 50 μM. In Vivo: Mirogabalin besylate (3 and 10 mg/kg) markedly increases AUC0-8 hours values in a dose-dependent manner in partial sciatic nerve ligation model rats. Mirogabalin (2.5, 5, and 10 mg/kg) causes significant and dose-dependent increase in AUC0-12 hours values and enhances analgesic effects, with estimated ED50 of 4.4, 3.1, and <2.5 mg/kg on day 1, day 3, and day 5, respectively. Moreover, Mirogabalin besylate shows no obvious effect on rota-rod performance and locomotor activity at 3 and 10 mg/kg via oral administration, exhibits significant inhibition on rota-rod performance at 10, 30, and 100 mg/kg, and decreases locomotor activity at 30 and 100 mg/kg in rats. 相关产品：Bioactive Compound Library Plus | Membrane Transporter/Ion Channel Compound Library | Neuronal Signaling Compound Library | Orally Active Compound Library | Neuroprotective Compound Library | Mechanoreceptors Compound Library | Calcium Channel Blocker Library | Antihypertensive Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Ion Channel Compound Library | Bioactive Compound Library Max | Thapsigargin | Ionomycin | L-Ascorbic acid | Minocycline hydrochloride | Verapamil | 2-Aminoethyl diphenylborinate | Acetylcholine chloride | GSK1016790A | Nifedipine | Fasudil Hydrochloride | Ebselen | Halofuginone | Bay K 8644 | Carbamazepine | Tetrandrine | Ruthenium red | L-Phenylalanine | ISX-9 | Gabapentin | Amlodipine | CDN1163 | TPC2-A1-N | Ethacrynic acid | Cromolyn sodium | Dantrolene | Diltiazem hydrochloride | Taurolithocholic acid sodium salt 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。