货号	规格	价格	上海	北京	珠海	南京	武汉
S88276-5mg一口价	≥98%	￥690.00 ￥552.00 S88276-5mg ￥552.00 现货	200 >10	-	-	-	-
S88276-10mg	≥98%	￥1090.00 S88276-10mg ￥1090.00 现货	100 >10	-	-	-	-
S88276-25mg	≥98%	￥1990.00 S88276-25mg ￥1990.00 现货	40 >10	-	-	-	-
S88276-50mg	≥98%	￥3090.00 S88276-50mg ￥3090.00 现货	20 >10	-	-	-	-
S88276-100mg	≥98%	￥4990.00 S88276-100mg ￥4990.00 现货	10 10	-	-	-	-

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产品描述：

Mirogabalin besylate is a selective and orally available 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

靶点：

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

体外研究：

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

体内研究：

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

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.721 ml	13.607 ml	27.214 ml
5 mM	0.544 ml	2.721 ml	5.443 ml
10 mM	0.272 ml	1.361 ml	2.721 ml
50 mM	0.054 ml	0.272 ml	0.544 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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