Absorption, Distribution and Excretion
Following a single oral administration of 10 mg/kg [phenyl-U-(14)C]-NF-114 to rats, no sex-related differences were observed in absorption, metabolism, distribution, or excretion. Peak plasma radioactivity was reached within 1 hour of administration in both male and female rats. Low levels of radioactivity were detected in all tissue, organ, and blood samples. Radioactivity in urine accounted for 69.5–74.4% of the administered dose, and in feces, 21.7–21.9%. /From Table/ Males and Females: Single Oral Administration of 10 or 300 mg/kg: Approximately 93.8–100.6% of the administered dose was recovered after oral administration of [phenyl-U-(14)C]-NF-114 to rats. Urine was the primary route of excretion. Low levels of radioactivity were detected in all tissue, organ, and blood samples collected 2 days (10 mg/kg group) or 4 days (300 mg/kg group) after administration, with higher concentrations in male tissues compared to females. The excretory metabolite profiles were similar in both quantity and quality across sex and dose groups. /Excerpt from Table/

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Metabolism/Metabolites
The metabolism of trifluimidazole was investigated by analyzing fecal and urine samples collected from previous studies: single oral doses of 10 or 300 mg/kg body weight, and 10 mg/kg body weight daily for 14 consecutive days. …Trifluimidazole is extensively metabolized: less than 2% of the radiolabeled substances recovered from urine or feces were identified as the parent compound. Some differences in metabolite patterns were observed between men and women after repeated low-dose and single high-dose administration, but no differences were observed after a single low-dose administration. The major metabolites in urine were sulfate conjugates of FM-8-1 and FA-1-5, accounting for approximately 20% of the radiolabeled radionuclide recovered from the matrix after a single low-dose administration, and approximately 11% and 20%, respectively, after a high-dose administration. In feces, FD-2-1 was the major metabolite across all dosing regimens (accounting for approximately 6-10% of the recovered radiolabeled radionuclide). Other major metabolites varied significantly across dosing regimens. FM-2-1 was the major metabolite after a single oral low-dose administration (accounting for approximately 9% of the recovered radiolabeled radionuclide in feces), but accounted for less than 2% in other dosing regimens. FA-1-1 was the major metabolite after single and repeated low-dose administrations (approximately 5-10%), but not significantly after a single oral high-dose administration (<3%); while FD-1-1 was the major metabolite after a single oral high-dose administration (approximately 16%), but a minor metabolite after single and repeated low-dose administrations (<2%). The metabolite FM-6-1 was preliminarily identified by thin-layer chromatography cochromatography, but due to its low radioactivity, the radioactive band corresponding to the standard FM-6-1 was not obvious.

Toxicity Summary
Identification and Uses: Trifluimidazole is a fungicide used to control powdery mildew, such as Sphaerotheca fuliginea, Sphaerotheca pannosa, and Erysiphe cichoracearum. Human Exposure and Toxicity: A report has been published detailing the annual health check results of personnel involved in trifluimidazole production at the Takaoka Plant in Japan from May 1996 to May 2002. No adverse health reactions related to chemical exposure were observed. Furthermore, the report states that no acute poisoning or skin and/or eye irritation events due to contact were observed during the reported period. Repeated or prolonged exposure may cause skin sensitization. This substance may affect the liver and blood, potentially leading to liver dysfunction and decreased hemoglobin levels. Animal Studies: Trifluimidazole has a sensitizing effect on guinea pig skin and a mild eye irritant effect on rabbits. Acute inhalation toxicity tests of trifluimidazole were conducted on rats. Most animals exhibited toxic symptoms, including arched back, lethargy, and lacrimation (head and/or nose). Oral administration of trifluimidazole to rats resulted in ataxia, hypotonia, lateral decubitus position, lacrimation, urinary incontinence, hypothermia, decreased heart and respiratory rates, and ptosis. Trifluimidazole treatment for 104 weeks did not induce tumors in rats. In rat developmental studies, no statistically significant external, visceral, or skeletal malformations or variations associated with treatment were observed. In mouse studies, prenatal exposure to trifluimidazole increased adipose tissue weight and promoted the differentiation of mesenchymal stem cells into adipocyte lineages. Trifluimidazole did not show mutagenicity in the Ames assay, regardless of metabolic activation. Ecotoxicity studies: The developmental toxicity of five commonly used triazole fungicides, including trifluimidazole, was evaluated using the rare early-life-stage goby (Gobiocypris rarus), revealing extremely high toxicity.

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Non-human toxicity values
Oral LD50 in rats: 2230 mg/kg (Terraguard 50W)
Oral LD50 in male rats: 1057 mg/kg body weight
Oral LD50 in female rats: 1780 mg/kg body weight
Inhalation LC50 in rats: >3.6 mg/L/4 hours
For more non-human toxicity values (complete data) for trifluimidazole (6 items in total), please visit the HSDB record page.

[1]. Acute toxicity of triflumizole to freshwater green algae Chlorella vulgaris. Pestic Biochem Physiol. 2019 Jul;158:135-142.

Triflumizole is a carboxymididine compound formed by the condensation of the amino group of 4-chloro-2-(trifluoromethyl)aniline with the acetyl oxygen atom of N-(propoxyacetyl)imidazole. It is a sterol demethylase inhibitor and can be used as a fungicide to control powdery mildew, scab, and other diseases on various crops. It is an EC 1.14.13.70 (sterol 14α-demethylase) inhibitor and antifungal pesticide. It belongs to the monochlorobenzene, imidazole, (trifluoromethyl)benzene, carboxymididine, ether, azole fungicides, and imidazole fungicides.

C15H15CLF3N3O

345.75

345.085

68694-11-1

91699

Colorless crystals

1.3±0.1 g/cm3

421.2±55.0 °C at 760 mmHg

63.5°C

208.6±31.5 °C

0.0±1.0 mmHg at 25°C

1.533

4.66

0

6

6

23

406

0

CCCOC/C(=N\C1=C(C=C(C=C1)Cl)C(F)(F)F)/N2C=CN=C2

HSMVPDGQOIQYSR-UHFFFAOYSA-N

InChI=1S/C15H15ClF3N3O/c1-2-7-23-9-14(22-6-5-20-10-22)21-13-4-3-11(16)8-12(13)15(17,18)19/h3-6,8,10H,2,7,9H2,1H3

N-[4-chloro-2-(trifluoromethyl)phenyl]-1-imidazol-1-yl-2-propoxyethanimine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)