Alosetron Hydrochloride (Synonyms: GR 68755) |
| Catalog No.GC11166 |
A 5-HT3 receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 122852-69-1
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Synonyms | GR 68755 | ||
| Chemical Name | 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 | ||
| Formula | C17H19ClN4O | M.Wt | 330.81 |
| Solubility | Insoluble in DMSO, ≥ 46.4 mg/mL in Water with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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