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Ondansetron [99614-02-5]

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Referencia NB-64-35292-200mg

embalaje : 200mg

Marca : Neo Biotech

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Ondansetron

(Synonyms: SN 307, GR-C507/75, GR 38032F, GR 38032) Copy Product Info

Synonyms: SN 307, GR-C507/75, GR 38032F, GR 38032

Catalog No. T6615 Copy Product Info

Purity: 99.92%

Ondansetron (GR 38032) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.

Cas No. 99614-02-5

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.92%

Appearance:Solid

Color:White

Product Information

Ondansetron AI Summary

Ondansetron exhibits a variety of bioactivities primarily related to its high affinity for the 5-hydroxytryptamine 3 (5-HT3) receptor. It demonstrates potent antagonist activity against this receptor, with Ki values as low as 0.77 nM and IC50 values in the range of 1.4 to 1.95 nM in different assays. This compound effectively inhibits 5-HT3 receptor-induced responses, such as bradycardia and emesis, with significant efficacy in both in vitro and in vivo models. For instance, it exhibits an ID50 of 0.0036 mg/kg for inhibiting 5-HT-evoked reflex bradycardia in rats, and an ED50 of 0.008 mg/kg intravenously for reducing cisplatin-induced emetic episodes in ferrets and dogs. Additionally, Ondansetron has shown various degrees of inhibitory activity against other receptors and enzymes. It displays weak binding affinities for receptors such as dopamine D2, 5-HT1, and 5-HT2, with Ki values greater than 1000 nM. The compound also shows moderate effectiveness in inhibiting human liver transporters (e.g., OCT1, HERG, BSEP) and enzymes, with IC50 values ranging from 400 nM to greater than 135,000 nM. Furthermore, in pharmacokinetic evaluations, Ondansetron has an oral bioavailability of 79%, a volume of distribution at steady state (Vdss) of 1.8 L/kg, and demonstrates a hepatic clearance rate of 5.8 mL/min/kg. It also exhibits an unbound fraction of 0.27 in human plasma and a half-life (T1/2) of 3.4 hours after intravenous administration in humans. In terms of therapeutic relevance, Ondansetron has exhibited antiemetic properties and antidepressant-like activities in animal models, as well as minimal hepatotoxic effects. However, it has limited efficacy against specific viruses, including SARS-CoV-2, with antiviral assay results indicating low effectiveness. Overall, Ondansetron’s primary pharmacological action is as a potent antagonist of the 5-HT3 receptor, making it a potential candidate for treating conditions such as chemotherapy-induced nausea and vomiting, with additional relevance in various serotonin-related physiological functions..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Ondansetron (GR 38032) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.
Targets & IC50	5-HT:103 pM
Synonyms	SN 307, GR-C507/75, GR 38032F, GR 38032

Chemical Properties

Molecular Weight	293.36
Formula	C₁₈H₁₉N₃O
Cas No.	99614-02-5
Smiles	Cl.CN1C2=C(C3=CC=CC=C13)C(=O)C(CN1C=CN=C1C)CC2
Relative Density.	1.27 g/cm3

Storage & Solubility Information

Storage

Keep away from direct sunlight, Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 4.4 mg/mL (15 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.41 mM), Sonication is recommended.

10% DMSO+90% Saline: 0.44 mg/mL (1.5 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.4088 mL	17.0439 mL	34.0878 mL	170.4391 mL
5 mM	0.6818 mL	3.4088 mL	6.8176 mL	34.0878 mL
10 mM	0.3409 mL	1.7044 mL	3.4088 mL	17.0439 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

SN-307SN307Serotonin ReceptorOndansetronInhibitorinhibitGR-38032GR380325-hydroxytryptamine Receptor5HTReceptor5-HT35-HT Receptor5HT Receptor5-HT

Related Tags: Ondansetron chemical structure | Ondansetron formula | Ondansetron molecular weight