Flumexadol |
Catalog No.GC38912
One-Click Copy Product Info
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Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 30914-89-7
Sample solution is provided at 25 µL, 10mM.
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Flumexadol is an orally active non-narcotic analgesic. Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor[1][2].
In rats and dogs dosed with 14C-Flumexadol (CERM1841), the 14C is excreted in the urine. The 14C eliminated in the faeces of dog is significantly higher than for rat. Conjugated metabolites, mostly glucuronides, accounted for the greater part of the urinary radioactivity in both species. Biotransformation products are predominantly acids in both species, follows by significant amounts of basic metabolites, with very little neutral substances. The major urinary metabolite in rats is 3-trifluoromethylbenzoic acid and 3-trifluoromethylhipuric acid. In the dog it is 3-trifluoromethylmandelic acid in addition to 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 first predominating[3].
[1]. Hache J, et al. The pharmacology of 1841 CERM, a new analgesic. Arzneimittelforschung. 1978;28(4):642-5. [2]. Nilsson BM. 5-Hydroxytryptamine 2C (5-HT2C) receptor agonists as potential antiobesity agents. J Med Chem. 2006 Jul 13;49(14):4023-34. [3]. Kucharczyk N, et al. Metabolites of 2-(3-trifluoromethylphenyl)tetrahydro-1,4-oxazine (CERM) 1841) in rats and dogs. Xenobiotica. 1979 Nov;9(11):703-11.
| Cas No. | 30914-89-7 | SDF | |
| Canonical SMILES | FC(C1=CC(C2CNCCO2)=CC=C1)(F)F | ||
| Formula | C11H12F3NO | M.Wt | 231.21 |
| Solubility | DMSO: 100 mg/mL (432.51 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.3251 mL | 21.6254 mL | 43.2507 mL |
| 5 mM | 865 μL | 4.3251 mL | 8.6501 mL |
| 10 mM | 432.5 μL | 2.1625 mL | 4.3251 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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 saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)