Mirogabalin besylate (DS 5565 besylate)
(Synonyms: 10928苯磺酸盐,DS 5565 besylate) 目录号 : GC30961
A calcium channel blocker
Cas No.:1138245-21-2
Sample solution is provided at 25 µL, 10mM.
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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)
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. | |
| Cas No. | 1138245-21-2 | SDF | |
| 别名 | 10928苯磺酸盐,DS 5565 besylate | ||
| Canonical 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 |
| 溶解度 | DMSO : 125 mg/mL (340.17 mM) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7214 mL | 13.6069 mL | 27.2138 mL |
| 5 mM | 0.5443 mL | 2.7214 mL | 5.4428 mL |
| 10 mM | 0.2721 mL | 1.3607 mL | 2.7214 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet