Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Mirogabalin besylate is a potent and orally active ligand that selectively targets the α2δ subunit of voltage-gated calcium channels. It displays high affinity (K d ) values, namely 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.
产品描述 | Mirogabalin besylate is a potent and orally active ligand that selectively targets the α2δ subunit of voltage-gated calcium channels. It displays high affinity (K d ) values, namely 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. |
体外活性 | Mirogabalin besylate is a ligand for the α2δ subunit of voltage-gated calcium channels, with K d s 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 IC 50 value of 16.0 nM. Mirogabalin has no effect on any other receptors, channels, transporters, or enzymes at 50 μM [1]. |
体内活性 | 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 AUC 0-12 hours values and enhances analgesic effects, with estimated ED 50 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 [1]. |
分子量 | 367.46 |
分子式 | C18H25NO5S |
CAS No. | 1138245-21-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Mirogabalin besylate 1138245-21-2 Inhibitor inhibitor inhibit