Alosetron Hydrochloride
(Synonyms: 盐酸阿洛司琼,GR 68755C;GR 68755;GR 68755X;Lotronex;GR-68755;GR68755) 目录号 : GC11166
A 5-HT3 receptor antagonist
Cas No.:122852-69-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Alosetron Hydrochloride (GR 68755 Hydrochloride) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.IC50 Value: Target: 5-HT ReceptorAlosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract. While being a 5-HT3 antagonist like ondansetron, it is not classified or approved as an antiemetic. Since stimulation of 5-HT3 receptors is positively correlated with gastrointestinal motility, alosetron's 5-HT3 antagonism slows the movement of fecal matter through the large intestine, increasing the extent to which water is absorbed, and decreasing the moisture and volume of the remaining waste products. From Wikipedia.
References:
[1]. Targeting the 5-HT3 receptor in the treatment of irritable bowel syndrome By Spiller, Robin C. From Current Opinion in Pharmacology (2011), 11(1), 68-74.
[2]. Lucak SL.Optimizing outcomes with alosetron hydrochloride in severe diarrhea-predominant irritable bowel syndrome.Therap Adv Gastroenterol. 2010 May;3(3):165-72.
[3]. Lewis JH.Alosetron for severe diarrhea-predominant irritable bowel syndrome: safety and efficacy in perspective.Expert Rev Gastroenterol Hepatol. 2010 Feb;4(1):13-29.
[4]. Turgeon DK, Tayeh N, Fontana RJ.Acute hepatitis associated with alosetron (Lotronex).J Clin Gastroenterol. 2005 Aug;39(7):641-2.
[5]. Miller DP, Alfredson T, Cook SF, Sands BE, Walker AM.Incidence of colonic ischemia, hospitalized complications of constipation, and bowel surgery in relation to use of alosetron hydrochloride.Am J Gastroenterol. 2003 May;98(5):1117-22.
| Cas No. | 122852-69-1 | SDF | |
| 别名 | 盐酸阿洛司琼,GR 68755C;GR 68755;GR 68755X;Lotronex;GR-68755;GR68755 | ||
| 化学名 | 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one;hydrochloride | ||
| Canonical SMILES | CC1=C(N=CN1)CN2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl | ||
| 分子式 | C17H19ClN4O | 分子量 | 330.81 |
| 溶解度 | Insoluble in DMSO, ≥ 46.4 mg/mL in Water with gentle warming | 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 | 3.0229 mL | 15.1144 mL | 30.2288 mL |
| 5 mM | 0.6046 mL | 3.0229 mL | 6.0458 mL |
| 10 mM | 0.3023 mL | 1.5114 mL | 3.0229 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。