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 K_d 值分别为 13.5 nM，22.7 nM，27 nM 和 47.6 nM。

Mirogabalin besylate is a selective and orally available 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.

Solid

Kd: 13.5 nM (Human α2δ-1), 22.7 nM (Human α2δ-2), 27 nM (Rat α2δ-1), 47.6 nM (Rat α2δ-2)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Domon Y, et al. Binding Characteristics and Analgesic Effects of Mirogabalin, a Novel Ligand for the α2δ Subunit of Voltage-Gated Calcium Channels. J Pharmacol Exp Ther. 2018 Jun;365(3):573-582.

In Vitro: DMSO : 125 mg/mL (340.17 mM; Need ultrasonic)配制储备液