| Description | Rimegepant (BMS 927711) is a potent calcitonin gene-related peptide (CGRP) receptor antagonist (Ki=0.027 nM, IC50=0.14 nM). Rimegepant can be used for the treatment of acute attacks of migraine as well as for prophylaxis. |
| In vitro | 方法：转染人 CGRP 受体的 Cos7 细胞用 αCGRP (10 nM) 和 Rimegepant (0.1 nM-10 µM) 处理 15 min，使用 cAMP Assay 检测 cAMP 水平。结果：Rimegepant 完全阻断 CGRP 受体的激活，pIC50 为 8.00 [10 nM]。[1]方法：人 NP 细胞用 Rimegepant (0.1-10 µM) 和 CGRP (1 µM) 处理 24 h，使用 CCK 8 assay 检测细胞活力。结果：Rimegepant 可以恢复 CGRP 介导的人类 NP 细胞中降低的细胞活力。[2] |
| In vivo | 方法：为检测对椎间盘退变 (IVDD) 的作用，将 Rimegepant (9 mg/kg) 口服给药给针刺损伤引起的 IVDD 小鼠模型，每天一次，持续一个月。结果：与假手术组相比，损伤组的椎间盘明显退化，而 Rimegepant 减轻了这种影响。免疫组织化学分析表明，与假手术组相比，损伤组 II 型胶原的蛋白质翻译减少。然而，与损伤组相比，损伤+ Rimegepant 组的小鼠显示 II 型胶原的蛋白质翻译恢复。[2] |
| Target activity | CGRP receptor:0.14 nM |
| Synonyms | BMS 927711, BMS-927711, BMS927711, BHV-3000 |
| molecular weight | 534.56 |
| Molecular formula | C28H28F2N6O3 |
| CAS | 1289023-67-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (93.53 mM) Ethanol: 10 mg/mL |
| References | 1. Pan KS, et al. Antagonism of CGRP Signaling by Rimegepant at Two Receptors. Front Pharmacol. 2020 Aug 20;11:1240. 2. Sun K, et al. CGRP Regulates Nucleus Pulposus Cell Apoptosis and Inflammation via the MAPK/NF-κB Signaling Pathways during Intervertebral Disc Degeneration. Oxid Med Cell Longev. 2021 Dec 26;2021:2958584. |
| Citations | 1. Sun K, Zhu J, Yan C, et al. CGRP Regulates Nucleus Pulposus Cell Apoptosis and Inflammation via the MAPK/NF-κB Signaling Pathways during Intervertebral Disc Degeneration. Oxidative Medicine and Cellular Longevity. 2021, 2021. 2. Jiang L, Zhou Y, Tang S, et al.Nociceptive adenosine A2A receptor on trigeminal nerves orchestrates CGRP release to regulate the progression of oral squamous cell carcinoma.International Journal of Oral Science.2024, 16(1): 46. |