Flufenoxuron (flufenoxuron)   中文名称: 氟虫脲

Absorption, Distribution and Excretion
/In rats/ Flufenoxuron exhibited a dose-dependant absorption following a single low dose (3.5 mg/kg) or single high dose (350 mg/kg). At the high dose, saturated absorption was observed. Approximately 86% of the low dose and 1% of the high dose was absorbed in 168 hours, the majority of which occurred within 48 hours. For the difluorobenzene ring test article, urine was a major route of excretion in the low-dose group, but not in the high-dose group (<1%). Conversely, 93-102% of the high dose and 4-19% of the low dose was eliminated in feces. Elimination via expired air was insignificant. Biliary excretion using the aniline ring label showed that all the radioactivity in the feces of females and 40% of that in males are biliary excretion products. Although, the majority of both urinary and fecal excretion occurred within 48 hours, excretion by both routes was biphasic, with slower phase occurring throughout the post-exposure, resulting in accumulation in adipose tissue. This phenomenon was probably due to entero-hepatic circulation. Accumulation of radioactivity in muscle and adipose tissue 4 hours post dosing with 3.5 mg/kg benzyl label was 30% and 42%, respectively. At 168 hours post dose, these values were 6% and 19%, respectively, suggesting an accumulation in the adipose tissue. High doses of both labels resulted in negligible tissue burden (<0.3%) indicating saturation absorption.

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Metabolism / Metabolites
Metabolism proceeds via hydrolysis to a benzoic acid and aryloxyphenylurea and aryoxyaniline moieties.
The metabolic fate of flufenoxuron was determined using two radiolabeled positions (aniline and difluorobenzene ring). Flufenoxuron exhibited a dose-dependant absorption following a single low dose (3.5 mg/kg) or single high dose (350 mg/kg). ... For the flufenoxuron aniline ring test article, the parent and a total of 10 urinary metabolites accounted for approximately 5% of the administered dose, and were considered non-significant. Fecal excretion of metabolites was quantitatively greater with parent compound accounting for the greatest portion of radioactivity. However, most fecal metabolites represented < 1% of the administered dose. Both [4-(2-chloro, alpha,alpah,alpha-trifluoro-p-tolyoxy)-2-fluorophenyl urea] and [4- (2-chloro, alpha,alpah,alpha-trifluoro-p-tolyoxy)-2-fluoroaniline] were detected in the feces and urine following administration of the aniline ring labeled test article. Unextractable residues accounted for 7-8% of the dose. The major urinary metabolite of [14C- 2,6-difluorobenzene]flufenoxuron was the corresponding benzoic acid which, over 48 hours, accounted for 10-12% of the administered dose. Difluorobenzamide (<1%) was also detected in the urine along with unknown components all of which individually represented <1% of the dose. The only component detected in the feces of rats given the 2,6-difluorobenzene label was the parent compound. The results of the metabolism characterization studies with both label positions suggest that metabolism of flufenoxuron proceeds via hydrolysis to a benzoic acid metabolite, a phenyl urea metabolite ( 4-[2-chloro, alpha,alpah,alpha-trifluoro-p-tolyoxy]-2-fluorophenyl urea), an aniline metabolite (4-[2-chloro, alpha,alpah,alpha-trifluoro-p-tolyoxy]-2-fluoroaniline), and subsequently several minor components.

Non-Human Toxicity Values
LC50 Rat inhalation >5.1 mg/L/4 hr
LD50 Mouse dermal > 2 g/kg
LD50 Rat dermal >2 g/kg
LD50 Rat oral >3 g/kg
For more Non-Human Toxicity Values (Complete) data for Flufenoxuron (6 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, a member of monochlorobenzenes, a member of (trifluoromethyl)benzenes, a member of monofluorobenzenes and a difluorobenzene. It has a role as a mite growth regulator. It is functionally related to a diphenyl ether.
Flufenoxuron is under investigation in clinical trial NCT00922870 (Evaluation of Hemodynamic Effects of Cascade Hemofiltration in Septic Shock).

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Mechanism of Action
Flufenoxuron is a benzoylurea type acaricide/insecticide which inhibits chitin biosynthesis (MOA Group 15) in nymphal mites and caterpillars.

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

67.43

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

注意： 本产品在运输和储存过程中需避光。

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)

配方 1 中的溶解度: ≥ 2.08 mg/mL (4.26 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (4.26 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。