Alosetron (Synonyms: GR 68755; GR 68755X)

Cat. No.: HY-70050A Purity: 96.26%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Alosetron (GR 68755) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC₅₀ at ~55 nM. Alosetron attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects.

For research use only. We do not sell to patients.

Alosetron Chemical Structure

CAS No. : 122852-42-0

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Other Forms of Alosetron:

Alosetron-d₃ hydrochloride In-stock
Alosetron Hydrochloride In-stock
Alosetron-d₃ Get quote
Alosetron (Hydrochloride(1:X)) Get quote
Alosetron ((Z)-2-butenedioate) Get quote

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

5-HT₃ Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	2.3 μM Compound: Alosetron	Inhibition of human ERG expressed in HEK cells by patch clamp technique Inhibition of human ERG expressed in HEK cells by patch clamp technique	[PMID: 20889341]

In Vivo

Dexamethasone and Alosetron-treated (1 mg/kg; ip; daily for 6 days) rats exhibits a significant decrease in the diarrhea index, in comparison with TNBS-control group, especially after the initial 2 days of treatment following the induction of colitis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

294.35

Formula

C₁₇H₁₈N₄O

CAS No.

122852-42-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(C(C1=C2C=CC=C1)=C(N2C)CC3)N3CC4=C(NC=N4)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (16.99 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3973 mL	16.9866 mL	33.9732 mL
5 mM	0.6795 mL	3.3973 mL	6.7946 mL
10 mM	0.3397 mL	1.6987 mL	3.3973 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 96.26%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (251 KB) HNMR (282 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Balfour JA, Goa KL, Perry CM. Alosetron. Drugs. 2000;59(3):511-520. [Content Brief]

[2]. Motavallian A, et al. Anti-inflammatory effects of alosetron mediated through 5-HT3 receptors on experimental colitis. Res Pharm Sci. 2019;14(3):228-236. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.3973 mL	16.9866 mL	33.9732 mL	84.9329 mL
	5 mM	0.6795 mL	3.3973 mL	6.7946 mL	16.9866 mL
	10 mM	0.3397 mL	1.6987 mL	3.3973 mL	8.4933 mL
	15 mM	0.2265 mL	1.1324 mL	2.2649 mL	5.6622 mL

Alosetron Related Classifications

Neurological Disease Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Alosetron122852-42-0GR 68755 GR 68755XGR68755GR-687555-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorselectivedepolarizationvisceralnociceptivecolitisInhibitorinhibitorinhibit

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