Methylnaltrexone Bromide
(Synonyms: Relistor) 目录号 : GC16177
Antagonist of peripherally acting μ-opioid
Cas No.:73232-52-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
-
Purity > 98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Methylnaltrexone Bromide is an antagonist of mu-opioid receptors (MOR) with IC50 value of 75nM.
MOR are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins. Activation of MOR in the intestinal tract inhibits peristaltic action which causes constipation [1].
In patients with constipation, Methylnaltrexone Bromide plus standard care relieved the constipation symptoms with less time (38 days) and improved quality life of 0.02 years or 8.8 days [1]. Methylnaltrexone is a novel MOR antagonist, which does not pass the blood brain barrier. In the first two weeks of usage, Methylnaltrexone Bromide caused laxation in less than 24 hours for at least half of those patients without impairing pain control or causing serious adverse effects. In phase II studies, all 22 patients had fast laxation [2].
References:
[1]. Earnshaw SR, Klok RM, Iyer S, et al. Methylnaltrexone bromide for the treatment of opioid-induced constipation in patients with advanced illness--a cost-effectiveness analysis. Aliment Pharmacol Ther, 2010, 31(8): 911-921.
[2]. Bader S, Jaroslawski K, Blum HE, et al. Opioid-induced constipation in advanced illness: safety and efficacy of methylnaltrexone bromide. Clin Med Insights Oncol, 2011, 5: 201-211.
| Cas No. | 73232-52-7 | SDF | |
| 别名 | Relistor | ||
| 化学名 | (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-3-ium-7-one;bromide | ||
| Canonical SMILES | C[N+]1(CCC23C4C(=O)CCC2(C1CC5=C3C(=C(C=C5)O)O4)O)CC6CC6.[Br-] | ||
| 分子式 | C21H26BrNO4 | 分子量 | 436.34 |
| 溶解度 | PBS (pH 7.2): 10 mg/ml | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2918 mL | 11.459 mL | 22.9179 mL |
| 5 mM | 0.4584 mL | 2.2918 mL | 4.5836 mL |
| 10 mM | 0.2292 mL | 1.1459 mL | 2.2918 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。