Absorption, Distribution and Excretion
... Rats dosed orally with radiolabelled trifluralin (14)C-CF3 or (14)C-N-propyl-; 100 mg/kg bw) excreted 80% of the dose in the feces; only 8% was unchanged trifluralin. Incomplete absorption was indicated by the finding that only 11-14% of the radioactivity was recovered from bile. ...
Four monkeys (2 males and 2 females) were administered 2 mg/kg radio-labeled ethalfluralin in ethanol intravenously or topically to the forearm and the plasma level determined for 120 hours to determine an area under the curve for both types of applications. ... After 120 hours label was not detectable in 2 (1 male and 1 female) of the 4 animals studied. Since the 2 animals with undetectable plasma levels at 120 hour yielded the most consistent data, data from these animals were used to calculate the AUCs. The dermal absorption was determined by ratio of the area under the plasma curve AUC; [(AUC-dermal/(AUC-i.v.)] x 100 = 2.84%. /Ethalfluralin/
Approx 80% of ingested compound was excreted in feces, remainder in urine /of rats & dogs studied/.

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Metabolism / Metabolites
Extensive nitro-reduction to the corresponding amines occurred, probably as a result of metabolism by the gut microflora. Absorbed trifluralin was extensively metabolized, primarily by N-dealkylation and nitro-reduction, and then excreted in the urine.
In a rat metabolism study, (14)C-trifluralin ( >98% radiochemical purity) in corn oil was administered by gavage at 300 mg/kg/day to 5 Fischer 344 rats/sex on three consecutive days. Metabolite characterization of the 24-48 hour urinary samples (pooled by sex) and quantitation of urinary samples collected at 0-24, 24-48, and 48-54 hours and pooled by sex were performed using liquid scintillation counting, silica gel column chromatography, TLC, HPLC, NMR, and mass spectroscopy. The objective of this study was to identify the urinary metabolites of trifluralin. There was no sex-dependent effect on metabolic profiles. A minimum of 20-30 non-conjugated metabolites and an additional 10-20 conjugated metabolites were present in the urine, but no parent compound was detected. Information on the percentage of the administered dose excreted in the urine was not provided. However, no single metabolite accounted for more than 8-10% of the total urinary radioactivity, and the majority of the metabolites were present at 1-2% of the total urinary radioactivity. Thus, almost all of the metabolites were minor (<5% of the total radioactive dose). Metabolite F1B was found at 8.2-8.9% of the total urinary radioactivity in both sexes, and Metabolite F2, N-((3-(acetylamino)-2-amino-5-(trifluoromethyl)) phenyl)acetamide, was found at 4.0-5.2%. Metabolite F1B was partially characterized as retaining the trifluoromethyl groups, the two equivalent aromatic protons, and the two nitro groups, but the propyl groups were lost. Ten other metabolites were identified (<0.1-3.7% of total urinary radioactivity, each compound in each sex). Two additional metabolites were partially characterized (0.1-2.6% of total urinary radioactivity, each compound in each sex). Four metabolic pathways were identified as follows: (i) oxidative N-dealkylation of one or both propyl groups and metabolites which were hydroxylated on the propyl side chain; (ii) reduction of one or both nitro groups to the corresponding amine; (iii) cyclization reactions to give a variety of substituted and unsubstituted benzimidazole metabolites; and (iv) conjugation reactions, including acetylation of the reduced nitro groups, sulfate, and glucuronic acid conjugates.
Major metabolites /found in urine & feces of treated ruminants/ were unidentified polar compounds, but N',N'-dipropyl-3-nitro-5-trifluoromethyl-ortho-phenylenediamine & N(4)N(4)-dipropyl-alpha,alpha,alpha-trifluorotoluene-3,4,5-triamine were also formed.
Trifluralin is dealkylated in rumen /of dairy animals/, losing 1 or both propyl groups; nitro groups are reduced to 1 or 2 amino groups. 2 types of reactions occur simultaneously, leading to a trifluoromethyltriaminobenzene.
For more Metabolism/Metabolites (Complete) data for TRIFLURALIN (6 total), please visit the HSDB record page.

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Biological Half-Life
Four monkeys (2 males and 2 females) were administered 2 mg/kg radio-labeled ethalfluralin in ethanol intravenously or topically to the forearm and the plasma level determined for 120 hours to determine an area under the curve for both types of applications. Two compartments were noted with one-half lives of 1.71 hours for the plasma distributive phase and 79.1 hours for the terminal plasma disappearance phase. ... /Ethalfluralin/
Salmon parr salmo salar were subjected to high initial concentrations of trifluralin & then maintained in clear water for 12 months. Some were removed at preselected intervals for exam by x-ray and chemical analysis. Half-life of trifluralin in salmon parr was 40.5 days.

Toxicity Data
LC50 (rat) = 2,800 mg/m3/1h

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Interactions
Mice were fed trifluralin at 1000, 1500 & 2000 ppm in diet for 12 or 14 weeks. Tumors were induced by admin 8 mg of benzo(a)pyrene orally at two time periods. Inhibition of tumorigenesis in lung & forestomach by trifluralin was observed when it was fed in diet 1 wk before or 1 day following exposure to benzo(a)pyrene.

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Non-Human Toxicity Values
LD50 Rat oral >10,000 mg/kg
LD50 Mouse oral 500 mg/kg
LD50 Rabbit oral >2000 mg/kg
LD50 Dog oral >2000 mg/kg
For more Non-Human Toxicity Values (Complete) data for TRIFLURALIN (11 total), please visit the HSDB record page.

Trifluralin is a yellow-orange crystalline solid. Denser than water and not soluble in water. Hence sinks in water. Melting point 48.5-49 °C. Used as a selective pre-emergence herbicide.
Trifluralin is a substituted aniline that is N,N-dipropylaniline substituted by a nitro groups at positions 2 and 6 and a trifluoromethyl group at position 4. It is an agrochemical used as a pre-emergence herbicide. It has a role as an environmental contaminant, a xenobiotic, a herbicide and an agrochemical. It is a C-nitro compound, a member of (trifluoromethyl)benzenes and a substituted aniline.
Trifluralin is used as a herbicide. No information is available on the acute (short-term), chronic (long- term), reproductive, developmental, or carcinogenic effects of trifluralin in humans. Decreased weight gain and effects on the blood and liver were observed in dogs chronically exposed to trifluralin in their diet. Skeletal abnormalities and depressed fetal weight were observed in the offspring of rodents exposed via gavage (experimentally placing the chemical in the stomach). Increased incidences of urinary tract tumors and thyroid tumors were observed in rats exposed to trifluralin in their diet. Trifluralin did not produce statistically significant increases in tumors in other studies. EPA has classified trifluralin as a Group C, possible human carcinogen (cancer-causing agent).
Trifluralin is a commonly used pre-emergence soil-incorporated herbicide. With about 14 million pounds used in the United States in 2001, it is one of the most widely used herbicides. Trifluralin is generally applied to the soil to provide control of a variety of annual grass and broadleaf weed species. It inhibits root development by interrupting mitosis, and thus can control weeds as they germinate. Its mode of action is selective and inhibits mitosis and cell division.
A microtubule-disrupting pre-emergence herbicide.

C13H16F3N3O4

335.28

335.109

1582-09-8

Trifluralin-d14;347841-79-6

5569

Pink to red solid powder

1.3±0.1 g/cm3

369.1±42.0 °C at 760 mmHg

48.5°C

177.0±27.9 °C

0.0±0.8 mmHg at 25°C

1.528

5.41

94.88

0

8

5

23

392

0

ZSDSQXJSNMTJDA-UHFFFAOYSA-N

InChI=1S/C13H16F3N3O4/c1-3-5-17(6-4-2)12-10(18(20)21)7-9(13(14,15)16)8-11(12)19(22)23/h7-8H,3-6H2,1-2H3

2,6-dinitro-N,N-dipropyl-4-(trifluoromethyl)aniline

Nitran; Elancolan; Trifluralin

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)

DMSO : ≥ 100 mg/mL (~298.26 mM)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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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。