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Itasetron

🥰Excellent
Catalog No. T24184Cas No. 123258-84-4
Alias UNII-00S0D0OEKR, U-98079A, U 98079A, DAU6215CL, DAU 6215CL

Itasetron (U 98079A) is a 5-hydroxytryptamine 3-receptor antagonist used to prevent age-related memory deficits in rats.Itasetron's antiemetic activity in animal models of cancer chemotherapy and radiation therapy may be useful in the study of amnesia.

Itasetron

Itasetron

🥰Excellent
Purity: 99.68%
Catalog No. T24184Alias UNII-00S0D0OEKR, U-98079A, U 98079A, DAU6215CL, DAU 6215CLCas No. 123258-84-4
Itasetron (U 98079A) is a 5-hydroxytryptamine 3-receptor antagonist used to prevent age-related memory deficits in rats.Itasetron's antiemetic activity in animal models of cancer chemotherapy and radiation therapy may be useful in the study of amnesia.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$147In StockIn Stock
5 mg$348In StockIn Stock
10 mg$475In StockIn Stock
25 mg$667In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.68%
ee:99.86%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Itasetron (U 98079A) is a 5-hydroxytryptamine 3-receptor antagonist used to prevent age-related memory deficits in rats.Itasetron's antiemetic activity in animal models of cancer chemotherapy and radiation therapy may be useful in the study of amnesia.
In vivo
Itasetron orally is rapidly absorbed (about 90 min), is highly bioavailable (greater than 90%), and has a long half-life (about 12 h). Itasetron (0.5, 1, 2, 4, and 8 mg; twice daily) in comparison with 8 mg b.i.d. ondansetron. Assessments were made in patients (n = 104) with histologically confirmed cancer (excluding head and neck tumors) and about to receive their first course of moderately emetogenic chemotherapy. Itasetron demonstrated comparable efficacy to ondansetron; no statistically significant between-group differences were observed in the primary (complete response rate) or secondary (nausea and delayed emesis) efficacy criteria. The tolerability of Itasetron was assessed as 'very good' or 'rather good' by 81% of patients and 89% of physicians. In conclusion, Itasetron is effective and well tolerated in patients receiving moderately emetogenic chemotherapy. Oral doses of 1 mg b.i.d. or above will be used in further clinical studies.[1]
SynonymsUNII-00S0D0OEKR, U-98079A, U 98079A, DAU6215CL, DAU 6215CL
Chemical Properties
Molecular Weight300.36
FormulaC16H20N4O2
Cas No.123258-84-4
SmilesC(N[C@H]1C[C@@]2(N(C)[C@](C1)(CC2)[H])[H])(=O)N3C=4C(NC3=O)=CC=CC4
Relative Density.1.35 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (149.82 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.3293 mL16.6467 mL33.2934 mL166.4669 mL
5 mM0.6659 mL3.3293 mL6.6587 mL33.2934 mL
10 mM0.3329 mL1.6647 mL3.3293 mL16.6467 mL
20 mM0.1665 mL0.8323 mL1.6647 mL8.3233 mL
50 mM0.0666 mL0.3329 mL0.6659 mL3.3293 mL
100 mM0.0333 mL0.1665 mL0.3329 mL1.6647 mL

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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