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Flumexadol

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Catalog No. T11302Cas No. 30914-89-7

Flumexadol is a selective 5-HT2C receptor agonist with an affinity (Ki) of 25 nM for the (+)-enantiomer and exhibits 40-fold selectivity over the 5-HT2A receptor. It is an orally active, non-narcotic analgesic.

Flumexadol

Flumexadol

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Catalog No. T11302Cas No. 30914-89-7
Flumexadol is a selective 5-HT2C receptor agonist with an affinity (Ki) of 25 nM for the (+)-enantiomer and exhibits 40-fold selectivity over the 5-HT2A receptor. It is an orally active, non-narcotic analgesic.
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Product Introduction

Bioactivity
Description
Flumexadol is a selective 5-HT2C receptor agonist with an affinity (Ki) of 25 nM for the (+)-enantiomer and exhibits 40-fold selectivity over the 5-HT2A receptor. It is an orally active, non-narcotic analgesic.
Targets&IC50
5-HT2C receptor:25 nM (ki)
In vivo
In rats and dogs dosed with 14C-Flumexadol (CERM1841), the 14C is primarily excreted in the urine. The 14C eliminated in the feces of dogs is significantly higher than that for rats. Conjugated metabolites, mostly glucuronides, accounted for the majority of the urinary radioactivity in both species. Biotransformation products are predominantly acids in both species, followed by substantial amounts of basic metabolites, with minimal neutral substances. The major urinary metabolites in rats are 3-trifluoromethylbenzoic acid and 3-trifluoromethylhippuric acid, whereas in dogs, the major metabolite is 3-trifluoromethylmandelic acid, along with the benzoic acid and its conjugate. The basic products identified in the urine of both species are unchanged drug and 1-amino-2-hydroxy-2-(3-trifluoromethylphenyl)ethane, with the former predominating.
Chemical Properties
Molecular Weight231.21
FormulaC11H12F3NO
Cas No.30914-89-7
SmilesFC(F)(F)c1cccc(c1)C1CNCCO1
Relative Density.1.2081 g/cm3 (Estimated)
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: 100 mg/mL (432.51 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (14.27 mM), Sonication is recommended.
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
1mg5mg10mg50mg
1 mM4.3251 mL21.6254 mL43.2507 mL216.2536 mL
5 mM0.8650 mL4.3251 mL8.6501 mL43.2507 mL
10 mM0.4325 mL2.1625 mL4.3251 mL21.6254 mL
20 mM0.2163 mL1.0813 mL2.1625 mL10.8127 mL
50 mM0.0865 mL0.4325 mL0.8650 mL4.3251 mL
100 mM0.0433 mL0.2163 mL0.4325 mL2.1625 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:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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