Flufenoxuron (flufenoxuron)   中文名称: 氟虫脲

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

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。