GLPBio

Alosetron ((Z)-2-butenedioate)

Catalog No.: GC35301Purity:>98%
Alosetron (GR 68755) (Z)-2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist.

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Alosetron ((Z)-2-butenedioate)
Cas No.: 122852-43-1
10mgIn Stock
$44.00
1
50mgIn Stock
$151.00
1

Citations

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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    31, 1291–1307 (2021)

Description

Alosetron (Z)-2-butenedioate (GR 68755 (Z)-2-butenedioate) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.IC50 Value: N/ATarget: 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.

[1]. Bleser S.Alosetron for severe diarrhea-predominant irritable bowel syndrome: improving patient outcomes.Curr Med Res Opin. 2011 Mar;27(3):503-12. [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]. Painsipp E, Shahbazian A, Holzer P.Alosetron, cilansetron and tegaserod modify mesenteric but not colonic blood flow in rats.Br J Pharmacol. 2009 Nov;158(5):1210-26. [5]. 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.

Chemical Properties

CAS No.
122852-43-1
SMILES
O=C(C(C1=C2C=CC=C1)=C(N2C)CC3)N3CC4=C(NC=N4)C.O=C(/C=C\C(O)=O)O
Molecular Formula
C21H22N4O5
Molecular Weight
410.42
Solubility
Soluble in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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