Ondansetron Hydrochloride Dihydrate

Catalog No.S4748

For research use only.

Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.

Ondansetron Hydrochloride Dihydrate Chemical Structure

CAS No. 103639-04-9

Purity & Quality Control

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Biological Activity

Description Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.
Targets
5-HT3 receptor [2]
810 nM
In vitro

Ondansetron is a potent, highly selective, competitive antagonist at 5-HT3 receptors. It demonstrates some affinity to other receptor subtypes, including 5-HT1B, 5-HT1C, 5-HT4, opioid, and 1-adrenergic receptors, and to the μ-opioid receptor. However, ondansetron has 1000:1 selectivity toward 5-HT3 receptors[1]. Ondansetron is found to be the most potent HERG-channel blocker among several 5-HT3 antagonists, with an IC50 of 810 nM and has been reported to block Na+ channels[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells NHLqZndHfW6ldHnvckBie3OjeR?= MmP3SIl{eGyjY3Xt[Y51KG:oIGuzTH1oemGwaYPleJJwdiCocn;tJIh2dWGwIEXIWFNCKHKnY3XweI9zKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[nliZnnseIVzKGKrbnTpcoch[XO|YYmsJGtqRTBwMECyPEDPxE1? MnHNNlE1QDZyM{i=
MDCK2 cells NFzvWHdHfW6ldHnvckBie3OjeR?= M2T2bmlvcGmkaYTpc44hd2ZiaIXtZY4hVUGWRUGtcYVlcWG2ZXSgX|E1ZS2vZYTmc5JucW5idYD0ZYtmKGW6cILld5Nm\CCrbjDwc4xiemm8ZXSgUWREUzJiY3XscJMh[W[2ZYKgOUBucW6|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5oKGGwYXz5d4l{NCCLQ{WwQVAvODFizszN MWWyN|I1OTB{OR?=
HEK cells NFf4ZmdHfW6ldHnvckBie3OjeR?= M4r2[GlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBJTUtiY3XscJMh[nlicHH0Z4gh[2yjbYCgeIVkcG6rcYXlMEBKSzVyPUCuOEDPxE1? MkntNlA5QDl|NEG=
CHO cells NIHl[2FHfW6ldHnvckBie3OjeR?= NVjKb2h5UW6qaXLpeIlwdiCxZjDoeY1idiCHUleg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTD3bI9t\SClZXzsJJBifGOqIHPsZY1xKHSnY3jubZF2\SxiSVO1NF0xNjhzMkizJO69VQ>? MUKxPFQ1QDN2Mh?=
In vivo Ondansetron(Ond) is well tolerated and its side effects are mild. Ond acts on the CNS as well as on the peripheral nervous system (PNS). Ondansetron is available both for oral and intravenous administration. The bioavailability of orally administered ondansetron is only 60%. The low bioavailability is due to a significant first-pass metabolism. The peak plasma concentration of ondansetron is usually reached at approximately 1.5 h after oral administration. A major portion of this drug, about 75%, is bound to plasma proteins. Ondansetron is currently used to prevent and treat nausea and vomiting associated with chemotherapy, radiation treatment and general anesthesia. It has been shown to inhibit GABA and glycine receptor activity in animal models[1]. Therapeutic dose of Ond allows delivery of significantly higher amounts of Dox to the brain tissue in vivo, which is otherwise disallowed by the BBB. The rate of penetration of the blood-brain barrier by Ond is very low[3].

Protocol (from reference)

Cell Research:[3]
  • Cell lines: PN1A and P1(0.5) cells; PSI-2, U87MG
  • Concentrations: 10 or 30 μg/ml
  • Incubation Time: 3 days
  • Method: Cells are plated in 60-mm Petri dishes (2×105 per dish) and cultured in serumcontained medium for 24 h. The next day the medium is removed and serum-contained medium with or without Dox (0.1 or 0.5 μg/ml) and Ond (10 or 30 μg/ml) in combination or respectively, is added. After 3 days, the cells are washed twice with PBS, trypsinized, and counted by using the trypan blue exclusion method.
Animal Research:[3]
  • Animal Models: Male adult Wistar rats
  • Dosages: 2 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 73 mg/mL warmed
(199.53 mM)
Water 73 mg/mL warmed
(199.53 mM)
Ethanol 40 mg/mL warmed
(109.33 mM)

Chemical Information

Molecular Weight 365.85
Formula

C18H19N3O.HCl.2H2O

CAS No. 103639-04-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.O.O.Cl

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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