For life science-related study, 1H-1,2,4-Triazol-3-amine is a biochemical reagent that can be utilized as an organic substance or biological material.

Absorption, Distribution and Excretion
Aminotriazole was applied to skin of rabbits. After 15 min it had penetrated into the blood. Fat was ... /an/ inconsequential site of storage.
Wistar rats were fed 1 mg 14C-amitrole (per rat) via stomach tube. The expired air, urine, feces and tissues were analyzed for radioactivity during a three day period following dosing. During the first 24 hours, 70 to 95.5% of the radioactivity was found in the urine; a small variable amount of activity was found in the feces. After absorption, amitrole was distributed throughout most body tissues. The maximum radioactivity was found in liver and kidney. Within three to four hours of dosing, the tissue levels began decreasing. Paper chromatography revealed both unchanged amitrole and one unidentified metabolite in rat liver slices taken at various times following dosing.
Primary routes of exposure are skin, eye contact and inhalation of powders, liquids, and sprays.
Anesthetized animals were allowed to inhale through a tracheal cannula liquid aerosols of drug solutions generated with an air-jet nebulizer. The aerosols had a mass median aerodynamic diameter of 2.81 um and a geometric standard deviation of 2.53. The time necessary for 50% absorption of amitrole was 1.3 min. Comparison with previously reported absorption rates measured after intratracheal injection of 0.1 mL of drug solution showed that drug inhaled as an aerosol was absorbed roughly 2 times more rapidly than when administered by intratracheal injection.
For more Absorption, Distribution and Excretion (Complete) data for AMITROLE (11 total), please visit the HSDB record page.

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Metabolism / Metabolites
After 39-yr-old woman ingested 20 mg/kg of aminotriazole, urine taken some hours later contained unchanged aminotriazole (100 mg/100 mL). No metabolites were found.
Metabolism... in plants: Glycine and serin of plants are utilized in biosynthesis of beta-(3-amino-S-triazolyl-1-)alpha-alanine.
In... studies with Canada thistle, 3 compounds ... observed. One was identified as beta-(3-amino-1,2,4-triazolyl-1)-alpha-alanine).
Major metabolic product formed from amitrole by microbiological activity was carbon dioxide. ... E coli converted 3-ATA into metabolite, 3-amino-1,2,4,-triazolyl alanine.
For more Metabolism/Metabolites (Complete) data for AMITROLE (10 total), please visit the HSDB record page.

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Biological Half-Life
Two groups of five male and five female Sprague-Dawley rats weighing 200-250 g were exposed (either nose only or whole body) to atmospheres of 5-14C-amitrole (radiochemical purity > 97%) in water aerosols at concentrations in air of 49.2 ug/liter (2.6 uCi/liter) or 25.8 ug/liter (1.4 uCi/liter), respectively, for 1 hr, and then observed for 120 hr. The particle size distribution of the aerosols was not reported. The calculated elimination half-life of radioactivity was approximately 21 hr for both exposures; approximately 75% of the radioactivity was eliminated in the urine within 12 hr.
Rats (5/sex; Charles River Ltd.) were exposed by inhalation to an estimated dose of 25.8 ug/L for "whole body" or 49.2 ug/L for "head only" radiolabelled amitrole for one hour. Blood samples were taken at specified intervals and urine, feces and carcasses were examined for radioactivity. ...The blood plasma half life was estimated to be 20 hours.

Toxicity Data
LC50 >500 mg/m3

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Interactions
... Effects on rat of 2 inhibitors ... on oxidation of methanol & ethanol to carbon dioxide, & on activities in vitro of rat-liver alcohol dehydrogenase & catalase. ... 3-amino-1,2,4-triazole considerably decreased ... carbon dioxide production from methanol ... & marginally ... from ethanol. ... There was additive effect ... when /used simultaneously with/ pyrazole ... .
3-amino-1,2,4-triazole administration (AT) at 3 and 6 hr led to the formation of round small vesicles from the rough endoplasmic reticulum, detachment of ribosomes, appearance of extensive areas of smooth endoplasmic reticulum, appearance of elongated and distorted mitochondria with an increase in the number of peroxisomes. The administration of carbon tetrachloride to AT-pretreated animals led to a mutual cancellation of the effects on the reticulum, & formation of myelin figures was prevented.
The placental transport of mercury in pregnant mice and its localization in the embryo and fetus from early organogenesis through the whole fetal period was studied by whole-body autoradiography and gamma counting. Preadmission to the dams of aminotriazole resulted in higher fetal concentration (esp in the liver) of mercury after inhalation of mercuric oxide but not after injection of (2+)mercury ion.
Inhalation of radioactive metallic mercury vapor in the mouse resulted in an accumulation of mercury in several organs where no specific uptake was observed after iv injection of inorganic mercury. Ethanol and aminotriazole (catalase inhibitors) decreased the concentration in several of these organs, although not in an exactly similar pattern. In the livers of non-treated animals most of the inhaled mercury accumulated in the hepatocytes in the periphery of the lobuli (periportal region), close to where the blood vessels enter the liver parenchyma. Treatment with aminotriazole increased the liver mercury content, with more or less all the hepatocytes apparently engaged in the oxidation of mercuric oxide.
For more Interactions (Complete) data for AMITROLE (9 total), please visit the HSDB record page.

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Non-Human Toxicity Values
LD50 Mouse oral 14.7 g/kg
LD50 Rat oral 25 g/kg
LD50 Mouse oral 11,000 mg/kg
LC50 Mouse inhalation 439 mg/cu m/4 hr
For more Non-Human Toxicity Values (Complete) data for AMITROLE (11 total), please visit the HSDB record page.

Amitrole can cause cancer according to an independent committee of scientific and health experts.
Amitrole appears as odorless white crystals or white powder. Bitter taste. Melting point 147-159 °C. Sublimes undecomposed at reduced pressure. Used as a post-emergence herbicide.
Amitrole is a member of the class of triazoles that is 1H-1,2,4-triazole substituted by an amino group at position 3. Used to control annual grasses and aquatic weeds (but not on food crops because it causes cancer in laboratory animals). Its use within the EU was banned from September 2017 on the grounds of potential groundwater contamination and risks to aquatic life; there have also been concerns about its endocrine-disrupting properties. It has a role as a herbicide, an EC 1.11.1.6 (catalase) inhibitor and a carotenoid biosynthesis inhibitor. It is an aromatic amine and a member of triazoles.
Amitrole is a colorless, odorless crystalline, aromatic amine with a bitter taste. Amitrole is a widely used herbicide for nonfood croplands to control annual and perennial grass type weeds, pondweeds and broad leaf. This substance has a very low acute toxicity in humans and is characterized by skin rash, diarrhea, nausea, vomiting and nose bleeds. Amitrole is reasonably anticipated to be a human carcinogen. (NCI05)
A non-selective post-emergence, translocated herbicide. According to the Seventh Annual Report on Carcinogens (PB95-109781, 1994) this substance may reasonably be anticipated to be a carcinogen. (From Merck Index, 12th ed) It is an irreversible inhibitor of CATALASE, and thus impairs activity of peroxisomes.

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Mechanism of Action
Amitrole inhibits peroxidase activity in liver & thyroids, & mode of action in producing thyroid tumors appears to be related to goitrogenic effect of amitrole with resultant increased TSH (thyroid-stimulating hormone) ... .
This study demonstrated that the compound 3-amino-1,2,4-triazole is a strong inhibitor of erythrocyte glutathione peroxidase activity. Moreover, 3-amino-1,2,4-triazole inhibits arachidonic-induced malondialdehyde formation in platelet-rich plasma and prostacyclin-like activity generation in aorta rings. These results give new lines of evidence on the connection between glutathione peroxidase activity and prostaglandin synthesis in rat platelets and arterial vessel walls.
A technique for the cytochemical demonstration of peroxidase activity in unfixed guinea-pig thyroid tissue is described. Both 3-amino-1,2,4-triazole and methimazole inhibited peroxidase activity in the follicle cells (enzyme activity was still seen in the erythrocytes), maximal inhibition occurring at 10 mmol.
Interference with histidine metabolism, inhibition of pigment biosynthesis, or both have been the principal candidates for the primary site of action of 3-amino-1,2,4-triazole (amitrole). Arabidopsis thaliana is sensitive to 1,2,4-triazole-3-alanine, a feedback inhibitor of histidine biosynthesis, and this effect is reversed by histidine. The combination of triazolealanine and histidine, however, does not reverse the herbicical effect of amitrole. This indicates that amitrole toxicity is not caused by histidine starvation, nor is it caused by the accumulation of a toxic intermediate of the histidine pathway. Amitrole inhibits root elongation at lower concentrations than it causes pigment bleaching in the leaves. In contrast, fluridone, a known inhibitor of the carotenoid biosynthetic pathway does not block root elongation. Fluridone also inhibits carotenoid accumulation in etiolated seedlings in the dark, but amitrole does not. Last, gabaculine and acifluorfen, but not amitrole, prevent chlorophyll accumulation in greeting etiolated seedlings of Arabidopsis. ...
For more Mechanism of Action (Complete) data for AMITROLE (8 total), please visit the HSDB record page.

C2H4N4

84.08

84.043

61-82-5

1639

Transparent to off white crystalline powder

1.8±0.1 g/cm3

85.4±23.0 °C at 760 mmHg

150-153 °C(lit.)

5.4±22.6 °C

69.5±0.2 mmHg at 25°C

1.823

-1.67

2

3

0

6

44.8

0

C1=NC(=N)NN1

KLSJWNVTNUYHDU-UHFFFAOYSA-N

InChI=1S/C2H4N4/c3-2-4-1-5-6-2/h1H,(H3,3,4,5,6)

1H-1,2,4-triazol-5-amine

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: 100 mg/mL (1189.34 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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