Glufosinate (1-100 μM; 12DIV) breaks down cell-cell adhesion in neural stem cells (NSC) of differentiated V-SVZ [2]. At 100 μM, glufosinate (1-100 μM; 12DIV) dramatically lowers Celsr2 gene expression [2]. The synthesis of cilia by ependymal cells is hindered by glutamate-ammonium [2].

In Wistar rats given dosages of 50 or 250 mg/kg, glufosinate-ammonium (10-250 mg/kg; gavage; daily; gestation days 6–15) showed maternal toxicity [3]. Less than four hours pass between the administration of glufosinate (oral intubation) and the blood of male and female rats [3].

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/

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.

[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…

C5H12NO4P

181.12688

181.05

51276-47-2

Glufosinate-d3 hydrochloride;1323254-05-2;Glufosinate ammonium;77182-82-2

4794

White to light yellow crystalline powder

1.378 g/cm3

519.1ºC at 760 mmHg

230ºC

267.7ºC

1.5

0.388

3

5

4

11

193

0

OC(C(CCP(=O)(C)O)N)=O

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

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

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.)