1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Flumexadol

Flumexadol 

Cat. No.: HY-133024 Purity: 98.50%
Handling Instructions

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.

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

Flumexadol Chemical Structure

Flumexadol Chemical Structure

CAS No. : 30914-89-7

Size Price Stock Quantity
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 115 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target[2]

5-HT2C Receptor

25 nM (Ki)

In Vivo

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].

Molecular Weight

231.21

Formula

C₁₁H₁₂F₃NO

CAS No.

30914-89-7

SMILES

FC(C1=CC(C2CNCCO2)=CC=C1)(F)F

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 : 100 mg/mL (432.51 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 provided by MCE.
References
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Keywords:

Flumexadol5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorNon-narcoticanalgesic5-HT2C5-HT2AInhibitorinhibitorinhibit

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Flumexadol
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HY-133024
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