GlpBio

Mirogabalin besylate (DS 5565 besylate)

目录号: GC30961纯度: >99.00%同义词: 10928苯磺酸盐,DS 5565 besylate

A calcium channel blocker

Mirogabalin besylate (DS 5565 besylate)
Cas No.: 1138245-21-2
规格价格库存数量操作
5mg¥630.00现货
1
10mg¥990.00现货
1
50mg¥2,790.00现货
1
100mg¥4,500.00现货
1
10mM (in 1mL DMSO)¥693.00现货
1
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文献被引

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    187(9):2288-2304 (2024)
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产品描述 Description

Mirogabalin is a calcium channel blocker with analgesic effects.1 It binds to the α2δ-1 and α2δ-2 subunits of voltage-dependent Ca2+ channels. Mirogabalin has potent and sustained analgesic effects (ED50 = 2.5 mg/kg) in rats with diabetes induced by streptozotocin . Mirogabalin does not inhibit activities associated with CNS adverse effects of analgesics, such as rotarod performance (ID50 = 9.4 mg/kg) or locomotor activity (ID50 = 43.9 mg/kg), at its effective dose.

1.Brown, K., Ohwada, S., Warren, V., et al.(405) A single ascending-dose study of mirogabalin in healthy subjects: Safety, tolerability, pharmacokinetic, and pharmacodynamic results.J. Pain17(4S)S76(2016)

实验参考方法 Experimental Reference Method

Animal experiment:

Rats[1]Eighty male rats are divided into groups of eight. After oral administration of Mirogabalin besylate (1, 3, 10, 30, and 100 mg/kg) or vehicle (control), locomotor activity is measured for 1 hour using the SUPERMEX system. Based on the time of peak effects of the test compounds (Mirogabalin besylate, etc.) in the rota-rod test, the pretreatment time is set at 6 hours for mirogabalin besylate and at 4 hours for pregabalin[1].

References:

[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.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
1138245-21-2
同义词
10928苯磺酸盐,DS 5565 besylate
SMILES
O=S(C1=CC=CC=C1)(O)=O.OC(C[C@@]2([C@@]3([H])[C@@](CC(CC)=C3)([H])C2)CN)=O
分子式
C18H25NO5S
分子量
367.46 g/mol
溶解性
DMSO : 125 mg/mL (340.17 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol