Absorption, Distribution and Excretion
Orally administered hexazinone has not been demonstrated to accumulate preferentially in any tissue. /Dose not specified/
... Hexazinone was given in the diet at 0, 1, 5, or 25 ppm to /dairy cows/ for 30 days. ... No detectable residues /were noted/ in milk, fat, liver, kidney or lean muscle.
...Three groups of male and female Sprague Dawley rats were treated as follows: (1) Group A received a single intragastric low dose of (14)C-hexazinone (14 mg/kg) without preconditioning (treatment with non-radioactive hexazinone); (2) Group B received a single intragastric dose of (14)C-hexazinone (14 mg/kg) after three weeks of preconditioning with 100 ppm of non-radioactive hexazinone in the diet; and (3) Group C received a single intragastric high-dose of (14)C-hexazinone (1000 mg/kg) without preconditioning. Hexazinone was rapidly metabolized by hydroxylation and demethylation, and eliminated by the rats in urine and feces during the 3 to 6-day testing periods. About 77% and 20% (of the administered dose) of (14)C-hexazinone was excreted in urine and feces, respectively. Practically all radioactivity was recovered in the first 24 hours after treatment. Very low levels of radioactivity (about 0.2% of the administered dose) were detected in the G.I. tract, hide, organs (heart, lungs, liver, spleen, kidneys, brain, and testes or ovaries), muscle, fat and blood.
/Male rats were/ ... administered 2,500 ppm (125 mg/kg) hexazinone in the diet ... for 17 days. This was followed by a single dose of 18.3 mg/300 g (61 mg/kg) (14)C-labeled hexazinone. The hexazinone was rapidly absorbed within 72 hours, with 61% detected in the urine and 32% in the feces. Trace amounts were found in the gastrointestinal tract (0.6%, tissues not specified) and expired air (0.08%).
For more Absorption, Distribution and Excretion (Complete) data for Hexazinone (8 total), please visit the HSDB record page.

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Metabolism / Metabolites
Major urinary metabolites of hexazinone in rats /includes the following/: 3-(4-hydroxycyclohexyl)-6-(dimethylamino)-1-methyl-1,3,5-triazine- 2,4-(1H,3H)-dione (metabolite A); 3-cyclohexyl-6-(methylamino)-1-methyl- 1,3,5-triazine-2,4-(1H,3H)-dione (metabolite B); and 3-(4-hydroxycyclohexyl)-6- (methylamino)-1-methyl-1,3,5-triazine-2,4-(1H,3H)-dione (metabolite C). The percentages of these metabolites detected in the urine were 46.8, 11.5 and 39.3%, respectively. The major fecal metabolites ... were A (26.3%) and C (55.2%). Less than 1% unchanged hexazinone was detected in the urine or the feces.

Toxicity Summary
IDENTIFICATION AND USE: Hexazinone is a white crystalline solid. It is used as an herbicide. HUMAN EXPOSURE AND TOXICITY: A 26-year-old woman inhaled hexazinone dust. Vomiting occurred within 24 hours. ANIMAL STUDIES: In a 10-day study dermal application of hexazinone for 6 hours/day for 10 days to male rabbits at 70 or 680 mg/kg/day resulted in no signs of skin irritation or toxicity. A trend toward elevated serum alkaline phosphatase (SAP) and serum glutamic pyruvic-transaminase (SGPT) activities was observed. Severe ocular irritant in rabbits. Rats fed 5000 ppm had growth curves slightly inferior to those of controls as the only detectable difference. Extending the feeding period to 2 yr produced decreased body weights in males fed 2500 ppm and in females fed either 1000 or 2500 ppm. All other indices of response, including the type and incidence of tumors, were similar in the test and control rats. Mice after 8 wk feeding up to 10,000 ppm produced increased liver weight only at the highest level without any other changes. 2 yr feeding of either 200, 2500, or 10,000 ppm resulted in sloughing of the distal tip of the tail and increased liver weights among mice fed 10,000 ppm. Hypertrophy of centrilobular hepatocytes and hyperplastic nodules were increased in mice fed either 2500 or 10,000 ppm. No evidence of a tumorigenic response was evident. Dogs fed 5000 ppm for 90 days had decreased rate of body weight gain with clinical signs of enzyme changes suggestive of liver damage. Microscopic examination of the liver failed to reveal any alterations and dogs fed 200 or 1000 ppm were indistinguishable from controls. No evidence of a teratogenic effect was seen in either rats or rabbits and reproduction capacity in rats fed up to 2500 ppm for three generations was unaffected. No carcinogenicity was detected among pups of rats fed up to 5000 ppm for 2 years. Similarly, no increase in tumors was produced by feeding up to 10,000 ppm hexazinone to mice. Hexazinone tested negative for mutagenicity in Salmonella typhimurium strains TA 1535, TA 1537, TA 1538, TA 98 and TA 100 at concentrations up to 7,000 ug/plate. ECOTOXICITY STUDIES: Two avian reproduction studies conducted show that the No Observed Effect Concentration (NOEC) for the bobwhite quail is <100 and for the mallard duck is >1000 ppm. Signal crayfish is more sensitive than the fish for hexazinone, and can be used as a bio-indicator of environmental contamination. Hexazinone was tested for its ability to control aquatic weeds when applied at 1.0 ppm in a 0.08 hectare pond. Dissolved oxygen declined from 8.0 ppm to 0.2 ppm within 5 days after treatment and appeared to be the cause of fish mortality observed 4 days post treatment.

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Non-Human Toxicity Values
LD50 Rat oral 860 mg/kg
LD50 Rat oral 1690 mg/kg
LD50 Rat dermal 5278 mg/kg
LD50 Guinea pig oral 860 mg/kg
For more Non-Human Toxicity Values (Complete) data for Hexazinone (9 total), please visit the HSDB record page.

[1]. Hexazinone.From Wikipedia.

Hexazinone is a white crystalline solid. Corrosive eye irritant. Used as an herbicide.
Hexazinone is a member of 1,3,5-triazines.
Hexazinone is an organic compound that is used as a broad spectrum herbicide. It is a colorless solid. It exhibits some solubility in water but is highly soluble in most organic solvents except alkanes. A member of the triazine class herbicides, it is manufactured by DuPont and sold under the trade name Velpar.

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Mechanism of Action
Inhibition of photosynthesis at photosystem II.

C12H20N4O2

252.3128

252.158

51235-04-2

Hexazinone-d6;1219804-22-4

39965

White to off-white solid powder

1.3±0.1 g/cm3

332.8±25.0 °C at 760 mmHg

97-100.5ºC

155.1±23.2 °C

0.0±0.7 mmHg at 25°C

1.612

1.85

60.13

0

2

2

18

386

0

CAWXEEYDBZRFPE-UHFFFAOYSA-N

InChI=1S/C12H20N4O2/c1-14(2)10-13-11(17)16(12(18)15(10)3)9-7-5-4-6-8-9/h9H,4-8H2,1-3H3

3-cyclohexyl-6-(dimethylamino)-1-methyl-1,3,5-triazine-2,4-dione

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

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。