Glufosinate-ammonium targets glutamine synthetase, a key enzyme in nitrogen metabolism. It inhibits this enzyme, leading to the accumulation of toxic levels of ammonia in plant cells, which ultimately causes plant death. It is a racemic mixture of D- and L-isomers.

In neural stem cells (NSCs), glufosinate (1-100 μM; 12DIV) destroys intercellular traces of secreted V-SVZ [2]. Celsr2 gene RT-PCR at 100 μM is significantly decreased by glufosinate (1-100 μM; 12DIV) [2].
In vitro, Glufosinate-ammonium inhibits glutamine synthetase activity. It is a potent inhibitor of this enzyme. Its herbicidal activity is based on this mechanism. It also has neurotoxic activity.

The maternal toxicity of 50 or 250 mg/kg of glufosinate (10-250 mg/kg; gavage; daily; on days 6–15 of gestation) was observed in Wistar rats [3]. In female musk deer, the half-life is shorter than 4 hours [3].
In vivo, Glufosinate-ammonium is effective as a herbicide for controlling a wide range of weeds. It is applied to plants, where it is absorbed and translocated, leading to plant death. It is also used as a desiccant.

In vitro enzyme/receptor binding assays for Glufosinate-ammonium involve measuring its inhibition of glutamine synthetase activity. These assays typically use purified enzyme preparations and appropriate substrates to determine the inhibitory potency.

RT-PCR [2]
Cell Types: Ependymal cells
Tested Concentrations: 1, 3, 10, 100 μM
Incubation Duration: 12DIV (NSCs -to) expression[2]. -Ependymal cell time point)
Experimental Results: Celsr2 gene expression was Dramatically diminished at 100 μM.
In vitro cell-based assays for Glufosinate-ammonium are not typically performed, as it is a herbicide. Its effects on plant cells are studied using whole-plant assays. Its neurotoxic effects may be studied in neuronal cell cultures.

In vivo animal experiments for Glufosinate-ammonium are not typically performed for herbicidal purposes. However, its toxicity has been studied in animals as part of safety assessments. It is a neurotoxin.

Metabolism / Metabolites
The main metabolite in urine and feces is 3-[hydroxy(methyl)phosphono]propionic acid. In plants, glufosinate degradation involves deamination, decarboxylation, and ultimately β-oxidation to produce carbon dioxide. Biological Half-Life …A 65-year-old male ingested BASTA containing 20% (w/v) glufosinate… The changes in serum glufosinate concentration showed a T_α of 1.84 hours and a T_β of 9.59 hours. /BASTA/
Glufosinate-ammonium is a highly soluble white to light yellow crystalline solid with a slightly pungent odor. Exposure occurs by inhalation, ingestion, or contact. Specific pharmacokinetic data is not provided.

Toxicity Summary
Glufosinate irreversibly inhibits glutamine synthase, thereby reducing ammonia detoxification capacity. Elevated ammonia levels lead to impaired photorespiration and photosynthesis in plants. (T10)

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Toxicity Data
LC50 (Rat) = 1,260 mg/m3

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Non-human Toxicity Values
LD50 Rats (Male) Oral 2000 mg/kg

LD50 Rats (Female) Oral 1620 mg/kg

Mouse (Male) Oral 431 mg/kg

Mouse (Female) Oral 416 mg/kg

For more non-human toxicity values (complete data) for glufosinate-ammonium salts (11 in total), please visit the HSDB records page.
Glufosinate-ammonium is a neurotoxin. It is a synthetic organophosphate compound. Its use as a pesticide is regulated due to its toxicity. It is characterized as a hazardous substance.

[1]. The effect of high concentrations of glufosinate ammonium on the yield components of transgenic spring wheat (Triticum aestivum L.) constitutively expressing the bar gene. ScientificWorldJournal. 2012;2012:657945.

[2]. Multiple effects of the herbicide glufosinate-ammonium and its main metabolite on neural stem cells from the subventricular zone of newborn mice. Neurotoxicology. 2018 Dec;69:152-163.

[3]. Summary of safety evaluation toxicity studies of glufosinate ammonium. Food Chem Toxicol. 1990 May;28(5):339-49.

2-Amino-4-[hydroxy(methyl)phosphoryl]butyric acid is a non-protein α-amino acid, formed by substituting a hydroxy(methyl)phosphoryl group at the 4-position of 2-aminobutyric acid. It belongs to the phosphonic acid class and is also a non-protein α-amino acid. Glufosinate is a metabolite found or produced in Escherichia coli (strains K12 and MG1655). Glufosinate has been reported to exist in Streptomyces hygroscopicus and Streptomyces viride, with relevant data available. Glufosinate or its ammonium salt DL-phosphinic acid is the active ingredient in many non-selective systemic herbicides, such as Basta, Rely, Finale, Ignite, Challenge, and Liberty. It interferes with the glutamine biosynthesis pathway, which binds to the glutamate binding site of the enzyme. Plants treated with glufosinate die due to ammonia accumulation and glutamine deficiency leading to the cessation of photosynthesis.

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Mechanism of Action
…Glufosinate is a structural analogue of glutamate, which exerts its effects in plants by inhibiting glutamine synthase, leading to the complete breakdown of ammonia metabolism. Due to the structural similarity between glufosinate and glutamate, its effects on various glutamate utilization systems in mammals need to be investigated. Although glufosinate inhibits glutamine synthase activity in different tissues in laboratory animals, this inhibition only leads to slight increases in glutamate and ammonia levels at high sublethal and lethal doses. After 28 days of oral administration, glufosinate had no effect on glutathione and carbohydrate metabolism, or on the biosynthesis of non-essential amino acids in rats and dogs. In vitro experiments showed that glufosinate does not interfere with multiple neurotransmitter receptors, and intravenous injection does not affect tissue concentrations of catecholamine neurotransmitters. These results indicate that…in mammals, inhibition of glutamine synthase activity in various tissues does not lead to the disruption of ammonia metabolism. Mammalian metabolism…compensates for the inhibition of glutamine synthase activity through various other metabolic pathways…
Glufosinate-ammonium is a broad-spectrum herbicide that inhibits glutamine synthetase. It is a neurotoxin and is used for total vegetation control. It is a racemic mixture and is not approved for medical use.

C5H15N2O4P

198.15

215.103

77182-82-2

Glufosinate;51276-47-2

4794

White to off-white solid powder

519.1ºC at 760 mmHg

210°C

100 °C

0.244

3

5

4

11

193

0

IAJOBQBIJHVGMQ-UHFFFAOYSA-N

InChI=1S/C5H12NO4P/c1-11(9,10)3-2-4(6)5(7)8/h4H,2-3,6H2,1H3,(H,7,8)(H,9,10)

2-amino-4-[hydroxy(methyl)phosphoryl]butanoic acid

HOE-00661; HOE 00661; Glufosinate-ammonium

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~250 mg/mL (~1261.61 mM)

Solubility in Formulation 1: 100 mg/mL (504.64 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

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