Maize microsomes metabolized rimsulfuron (DPX-E9636) in vitro in a process that required NADPH and produced the same hydroxylated product, indicating that cytochrome P450 was involved[1].

Absorption, Distribution and Excretion
In rats, limsulfuron was primarily excreted in urine (64%) and feces (30%) within 72 hours following administration. Low but detectable levels of radioactivity were detected in the heart, lungs, liver, kidneys, and muscles… This study investigated the metabolism of 14C-labeled limsulfuron in male and female rats. The low-dose group received 25 mg/kg of the 14C-pyridine-labeled compound via gavage, while the high-dose group received 250 mg/kg of either 14C-pyridine or 14C-pyrimidine-labeled compounds via gavage, respectively. The repeat-dose group received the unlabeled test compound (25 mg/kg) via gavage for 14 consecutive days, followed by a repeat gavage administration of 25 mg/kg of the 14C-pyridine-labeled test compound on day 15. 93% to 96% of the administered radioactive material was excreted, with 58% to 67% appearing in the urine and 20% to 33% in the feces. Tissue distribution of the labeled residue was minimal. In each experimental group, liver accumulation was slightly higher in males than in females. Mild accumulation was also observed in the spleen of animals in the repeat-dose groups. ... Metabolism/Metabolites Metabolism of limosulfuron in plants and other animals (poultry and ruminants) appeared similar to its metabolism in rats. Metabolism involves the contraction or cleavage of sulfonylurea bridges. Although cleavage to form pyridinesulfonamide metabolites was expected, the contraction response was uncommon. The main residue found in plants was the parent compound limosulfuron. This study investigated the metabolism of 14C-labeled limosulfuron in male and female rats. The low-dose group received 25 mg/kg of the 14C-pyridine-labeled compound via gavage, while the high-dose group received 250 mg/kg of either 14C-pyridine or 14C-pyrimidine-labeled compound via gavage. The repeat-dose group received the unlabeled test compound (25 mg/kg) via gavage for 14 consecutive days, followed by a second gavage administration of 25 mg/kg of the 14C-pyridine-labeled test compound on day 15. …Metabolic profiles were determined using mixed urine and fecal samples. The highest proportion of unmetabolized parent compound was observed in the radioactivity of urine (42%–55%) and feces (5%–16%). The parent compound undergoes metabolism via the cleavage or contraction of the sulfonylurea bridge to generate 3-(ethylsulfonyl)-2-pyridinesulfonamide (IN-E9260) or N-(4,6-dimethoxy-2-pyrimidinyl)-N-((3-ethylsulfonyl)-2-pyridinyl)urea (IN-70941). IN-70941 is deamidated to generate IN-70942, which is then subjected to demethylation and hydroxylation reactions to form IN-70942.

Non-Human Toxicity Values
Rabbit dermal LD50 >2000 mg/kg
Rat inhalation LC50 >5.4 mg/L/4 hr
Rat oral LD50 >5000 mg/kg
Mouse oral LD50 >5000 mg/kg
Rabbit dermal LD50 >2000 mg/kg

[1]. M.K.Koeppe, et al. Basis of Selectivity of the Herbicide Rimsulfuron in Maize.

Sulfuron is an N-sulfonylurea herbicide, chemically named N-carbamoyl-3-(ethylsulfonyl)pyridine-2-sulfonamide, in which the amino nitrogen atom is substituted with a 4,6-dimethoxypyrimidin-2-yl group. It is both an environmental pollutant and an exogenous substance and herbicide. Sulfuron belongs to the pyridine, N-sulfonylurea, pyrimidine, sulfone, and aromatic ether compounds. Sulfuron is a herbicide used to control annual grass and broadleaf weeds in corn, potatoes, and other crops. It is selective and systemic, absorbed through leaves and roots and transported into the plant. It is an acetolactate synthase (ALS) inhibitor. Mechanism of Action: …By inhibiting the plant enzyme acetolactate synthase, it blocks the synthesis of branched-chain amino acids.

C14H17N5O7S2

431.44

431.056

122931-48-0

Rimsulfuron-d6

91779

Colorless crystals

1.6±0.1 g/cm3

760.1±70.0 °C at 760 mmHg

172-177°C

413.5±35.7 °C

0.0±2.7 mmHg at 25°C

1.653

0.09

2

10

7

28

722

0

CCS(=O)(C1=C(S(=O)(NC(NC2=NC(OC)=CC(OC)=N2)=O)=O)N=CC=C1)=O

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: 33.33 mg/mL (77.25 mM)

Solubility in Formulation 1: ≥ 1.25 mg/mL (2.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 1.25 mg/mL (2.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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