Absorption, Distribution and Excretion
/In Rats/ Fluphenoxyurea exhibited dose-dependent absorption following a single low-dose (3.5 mg/kg) or single high-dose (350 mg/kg) administration. At the high dose, absorption saturation was observed. Approximately 86% of the drug in the low-dose group and approximately 1% in the high-dose group were absorbed within 168 hours, with the majority absorbed within 48 hours. For difluorobenzene ring test substances, urine was the primary route of excretion in the low-dose group, but this was not the case in the high-dose group (<1%). Instead, 93–102% of the drug in the high-dose group and 4–19% in the low-dose group were excreted in feces. Exhalation was negligible. Bile excretion assays using aniline ring labeling showed that all radioactivity in the feces of female rats and 40% in the feces of male rats were bile excretion products. Although most urinary and fecal excretion occurs within 48 hours, excretion via both routes is biphasic, with a slower phase occurring throughout the post-exposure period, leading to drug accumulation in adipose tissue. This phenomenon may be related to enterohepatic circulation. Four hours after administration of the 3.5 mg/kg benzyl-labeled drug, radioactive accumulation in muscle and adipose tissue was 30% and 42%, respectively. At 168 hours post-administration, these values were 6% and 19%, respectively, indicating drug accumulation in adipose tissue. High doses of both labels resulted in extremely low tissue load (<0.3%), indicating that absorption had reached saturation. Metabolism/Metabolites The metabolic pathway involves hydrolysis to benzoic acid, aryloxyphenylurea, and the aryloxyaniline moiety. The metabolic pathway of fluorophenoxyurea was determined using two radiolabeled sites (aniline and difluorophenyl ring). Fluoroxyurea absorption was dose-dependent following a single low-dose (3.5 mg/kg) or single high-dose (350 mg/kg) administration. …For the fluorophenoxyurea aniline ring test sample, the parent compound and a total of 10 urinary metabolites accounted for approximately 5% of the administered dose, which was considered insignificant. The excretion of metabolites in feces was significantly higher than in urine, with the parent compound exhibiting the largest radioactive proportion. However, most fecal metabolites accounted for less than 1% of the administered dose. [4-(2-chloro,α,α-trifluoro-p-tolyloxy)-2-fluorophenylurea] and [4-(2-chloro,α,α-trifluoro-p-tolyloxy)-2-fluoroaniline] were detected in both feces and urine after administration of the aniline ring-labeled test substance. Unretrievable residues accounted for 7-8% of the administered dose. The major urinary metabolite of [14C-2,6-difluorobenzene]fluorophenylurea was the corresponding benzoic acid, accounting for 10-12% of the administered dose over 48 hours. Difluorobenzamide (<1%) and some unknown components were also detected in urine, all of which individually accounted for <1% of the administered dose. In rat feces treated with the 2,6-difluorobenzene label, only the parent compound was detected. Metabolic characterization studies at both labeling sites indicated that the metabolism of fluorophenoxyurea proceeds via hydrolysis to produce benzoic acid metabolites, phenylurea metabolites (4-[2-chloro,α,α,α-trifluoro-p-tolyloxy]-2-fluorophenylurea), and aniline metabolites (4-[2-chloro,α,α,α-trifluoro-p-tolyloxy]-2-fluoroaniline), followed by the formation of several minor components.

Non-Human Toxicity Values
Rat inhalation LC50 > 5.1 mg/L/4 hr
Mouse dermal LD50 > 2 g/kg
Rat dermal LD50 > 2 g/kg
Rat oral LD50 > 3 g/kg
For more complete non-human toxicity data for flufenoxuron (6 in total), please visit the HSDB record page.

[1]. Toxic Effects of Flufenoxuron on Development and Vascular Formation During Zebrafish Embryogenesis. Aquat Toxicol. 2019 Nov;216:105307.

Flufenoxuron is a benzoylurea insecticide belonging to the monochlorobenzene, (trifluoromethyl)benzene, monofluorobenzene, and difluorobenzene compounds. It is a mite growth regulator, and its function is related to diphenyl ether compounds. Flufenoxuron is currently being studied in the clinical trial NCT00922870 (Evaluation of the hemodynamic effects of cascade hemofiltration in septic shock). Mechanism of Action: Flufenoxuron is a benzoylurea acaricide/insecticide that inhibits chitin biosynthesis in nymphs and caterpillars (mechanism of action group 15).

C21H11CLF6N2O3

488.77

488.036

101463-69-8

91766

Off-white to light yellow solid powder

1.5±0.1 g/cm3

169-172 °C (decomposes)

1.574

5.6

2

9

4

33

689

0

RYLHNOVXKPXDIP-UHFFFAOYSA-N

InChI=1S/C21H11ClF6N2O3/c22-12-8-10(21(26,27)28)4-7-17(12)33-11-5-6-16(15(25)9-11)29-20(32)30-19(31)18-13(23)2-1-3-14(18)24/h1-9H,(H2,29,30,31,32)

N-[[4-[2-chloro-4-(trifluoromethyl)phenoxy]-2-fluorophenyl]carbamoyl]-2,6-difluorobenzamide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

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

DMSO: 250 mg/mL (511.49 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (4.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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