Alosetron HCl
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MedKoo CAT#: 317171

CAS#: 122852-69-1 (HCl)

Description: Alosetron is a potent and selective 5-HT3 receptor antagonist. Alosetron blocks the actions of serotonin at 5-HT3 sites in the peripheral nervous system, particularly on enteric and nociceptive sensory neurons, thereby affecting the regulation of visceral pain, decreasing gastrointestinal contraction and motility, and decreasing gastrointestinal secretions. This agent is used to treat diarrhea-predominant irritable bowel syndrome in women only.


Chemical Structure

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Alosetron HCl
CAS# 122852-69-1 (HCl)

Theoretical Analysis

MedKoo Cat#: 317171
Name: Alosetron HCl
CAS#: 122852-69-1 (HCl)
Chemical Formula: C17H19ClN4O
Exact Mass: 294.14806
Molecular Weight: 330.816
Elemental Analysis: C, 61.72; H, 5.79; Cl, 10.72; N, 16.94; O, 4.84

Price and Availability

Size Price Availability Quantity
10.0mg USD 265.0 2 Weeks
25.0mg USD 450.0 2 Weeks
50.0mg USD 650.0 2 Weeks
100.0mg USD 950.0 2 Weeks
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Related CAS #: 122852-42-0 (free base)   122852-69-1 (HCl)    

Synonym: Alosetron HCl; Alosetron hydrochloride; Lotronex; GR68755; GR-68755; GR 68755;

IUPAC/Chemical Name: 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one hydrochloride

InChi Key: FNYQZOVOVDSGJH-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H18N4O.ClH/c1-11-13(19-10-18-11)9-21-8-7-15-16(17(21)22)12-5-3-4-6-14(12)20(15)2;/h3-6,10H,7-9H2,1-2H3,(H,18,19);1H

SMILES Code: O=C1N(CC2=C(C)NC=N2)CCC(N3C)=C1C4=C3C=CC=C4.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 330.816 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Cash BD, Lacy BE, Rao T, Earnest DL. Rifaximin and eluxadoline - newly approved treatments for diarrhea-predominant irritable bowel syndrome: what is their role in clinical practice alongside alosetron? Expert Opin Pharmacother. 2015 Dec 8:1-12. [Epub ahead of print] PubMed PMID: 26559529.

2: Chaudhary DV, Patel DP, Shah JV, Shah PA, Sanyal M, Shrivastav PS. Application of a UPLC-MS/MS method for the analysis of alosetron in human plasma to support a bioequivalence study in healthy males and females. Biomed Chromatogr. 2015 Oct;29(10):1527-34. doi: 10.1002/bmc.3454. Epub 2015 Mar 11. PubMed PMID: 25761551.

3: Tong K, Nicandro JP, Shringarpure R, Chuang E, Chang L. A 9-year evaluation of temporal trends in alosetron postmarketing safety under the risk management program. Therap Adv Gastroenterol. 2013 Sep;6(5):344-57. doi: 10.1177/1756283X13491798. PubMed PMID: 24003335; PubMed Central PMCID: PMC3756634.

4: Cremonini F, Nicandro JP, Atkinson V, Shringarpure R, Chuang E, Lembo A. Randomised clinical trial: alosetron improves quality of life and reduces restriction of daily activities in women with severe diarrhoea-predominant IBS. Aliment Pharmacol Ther. 2012 Sep;36(5):437-48. doi: 10.1111/j.1365-2036.2012.05208.x. Epub 2012 Jul 10. PubMed PMID: 22779693; PubMed Central PMCID: PMC3464357.

5: Lucak S. Irritable bowel syndrome and ischemic colitis: evidence supporting the increased use of alosetron. Therap Adv Gastroenterol. 2012 Jul;5(4):215-8. doi: 10.1177/1756283X12450934. PubMed PMID: 22778787; PubMed Central PMCID: PMC3388526.

6: Nicandro JP, Shin P, Chuang E. Evaluation of treatment continuation with alosetron by IBS-D severity criteria. Curr Med Res Opin. 2012 Mar;28(3):449-56. doi: 10.1185/03007995.2011.653435. Epub 2012 Feb 7. PubMed PMID: 22313141.

7: Bleser S. Alosetron for severe diarrhea-predominant irritable bowel syndrome: improving patient outcomes. Curr Med Res Opin. 2011 Mar;27(3):503-12. doi: 10.1185/03007995.2010.547933. Epub 2011 Jan 6. Review. PubMed PMID: 21208139.

8: Lucak SL. Optimizing outcomes with alosetron hydrochloride in severe diarrhea-predominant irritable bowel syndrome. Therap Adv Gastroenterol. 2010 May;3(3):165-72. doi: 10.1177/1756283X10362277. PubMed PMID: 21180598; PubMed Central PMCID: PMC3002579.

9: Chang L, Tong K, Ameen V. Ischemic colitis and complications of constipation associated with the use of alosetron under a risk management plan: clinical characteristics, outcomes, and incidences. Am J Gastroenterol. 2010 Apr;105(4):866-75. doi: 10.1038/ajg.2010.25. Epub 2010 Mar 2. PubMed PMID: 20197759.

10: 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. doi: 10.1586/egh.09.72. PubMed PMID: 20136586.