1. Anti-infection
    Metabolic Enzyme/Protease
  2. Fungal
    Cytochrome P450
  3. Mefentrifluconazole

Mefentrifluconazole 

Cat. No.: HY-136063 Purity: 99.86%
Handling Instructions

Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM).

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

Mefentrifluconazole Chemical Structure

Mefentrifluconazole Chemical Structure

CAS No. : 1417782-03-6

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 590 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2800 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

Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM)[1].

IC50 & Target[1]

CYP51A

0.5 nM (Kd)

In Vivo

Mefentrifluconazole undergoes extensive toxicity testing, including a full program of reproductive toxicity studies. Long term repeated dose toxicity and/or carcinogenicity studies have been conducted in rats, mice, and dogs. In each species, the highest dose level investigated gives rise to systemic toxicity[1].
In the acute and repeat dose toxicity studies performed with Mefentrifluconazole. A single-dose administration to rats the LD50 is >2000 mg/kg bwt by the oral route, >5000 mg/kg bwt by the dermal route, and >5.314 mg/L by inhalation as a dust aerosol. Mefentrifluconazole is not a skin or an eye irritant, nor is it a phototoxicant in vitro[1].
In the acute neurotoxicity study in rats, Mefentrifluconazole (oral administration; 2000 mg/kg bwt; single dose) gives rise to reduce body weight gain and transient neurobehavioral effects only on the day of treatment (unsteady gait, reduced motor activity, reduces grip strength of the forelimbs and increased distance between the hind limbs in the landing foot-splay test)[1].
In the repeated-dose toxicity studies, the liver is the target organ in each of the three species investigated. At higher dose levels in the rat (oral diets; 383/334 mg/kg/bwt/d (4000 ppm)) and the C57BL/6JRj mouse (61 mg/kg bwt/d (300 ppm)), reduces body weight gain and food consumption, alters clinical chemistry parameters, increases liver weight and is accompanied by liver cell hypertrophy, and/or liver cell necrosis. At low doses, increases liver weight is not associated with any histopathological alterations and is considered to be an adaptive change to treatment[1].

Molecular Weight

397.78

Formula

C₁₈H₁₅ClF₃N₃O₂

CAS No.

1417782-03-6

SMILES

OC(C)(C1=CC=C(OC2=CC=C(Cl)C=C2)C=C1C(F)(F)F)CN3N=CN=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -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 (251.40 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5140 mL 12.5698 mL 25.1395 mL
5 mM 0.5028 mL 2.5140 mL 5.0279 mL
10 mM 0.2514 mL 1.2570 mL 2.5140 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: ≥ 6.25 mg/mL (15.71 mM); Clear solution

  • 2.

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

    Solubility: ≥ 6.25 mg/mL (15.71 mM); Clear solution

  • 3.

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

    Solubility: ≥ 6.25 mg/mL (15.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.86%

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Keywords:

MefentrifluconazoleFungalCytochrome P450CYPsantifungallivercellhypertrophynecrosisirritantazolederivativearomataseInhibitorinhibitorinhibit

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Mefentrifluconazole
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