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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.


| 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. |
| Molecular Weight | 231.21 |
| Formula | C11H12F3NO |
| Cas No. | 30914-89-7 |
| Smiles | FC(F)(F)c1cccc(c1)C1CNCCO1 |
| Relative Density. | 1.2081 g/cm3 (Estimated) |
| Storage | Powder: -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
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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.
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.
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