[CAS NO. 30914-89-7]  Flumexadol

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PRODUCTS SPECIFICATIONS [30914-89-7]

Distributor
Catalog
AS186290
Brand
Arctom Scientific
CAS
30914-89-7

DESCRIPTION [30914-89-7]

Overview

MDLMFCD00864259
Molecular Weight231.21
Molecular FormulaC11H12F3NO
SMILESFC(C1=CC(C2CNCCO2)=CC=C1)(F)F

For research use only. We do not sell to patients.

Summary

Flumexadol is a selective and affinity 5-HT 2C receptor agonist with a K i of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT 2A receptor. Flumexadol is an orally active non-narcotic analgesic [1] [2] .


IC50 & Target

5-HT 2C Receptor

25 nM (Ki)


In Vivo

In rats and dogs dosed with 14 C-Flumexadol (CERM1841), the 14 C is excreted in the urine. The 14 C 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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Appearance

Liquid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL ( 144.15 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3251 mL 21.6254 mL 43.2507 mL
5 mM 0.8650 mL 4.3251 mL 8.6501 mL
10 mM 0.4325 mL 2.1625 mL 4.3251 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (10.81 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.81 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.81 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Morpholine, 2-[3-(trifluoromethyl)phenyl]-
2-[3-(Trifluoromethyl)phenyl]morpholine
1841CERM
2-(3-Trifluoromethylphenyl)morpholine
Flumexadol