Chlorfenuron is a commonly used plant growth regulator that makes kiwi fruits bigger and heavier. The Sulforhodamine B assay was used to investigate the cytotoxicity of clofenuron and its metabolites against CHO cells. An IC50 of 12.12±2.14 μM for chlorfenuron indicates considerable cytotoxicity to CHO cells[1]. Chlorfenuron has a half-life of 15.8–23.0 days. The pulp has a final residual chlorfenuron content of ≤0.002 mg/kg, with the peel containing the majority of the residue. According to the risk assessment, there is not a substantial risk to health associated with clofenuron found in citrus fruits. Consequently, it is safe to apply chlorfenuron on citrus fruits [2].

Absorption, Distribution and Excretion
In the primary and bile excretion studies, at least four Sprague-Dawley rats per pair of males and females were administered 100 mg/kg of CPPU-UL-phenyl-(14)C (radiochemical purity: 99.16%; specific activity: 28.04 mCi/mmol) by gavage, mixed with unlabeled chlorpyrifos technical (purity: 98.2%). In the primary study, urine, feces, and air samples were collected periodically over 7 days post-administration. In the bile excretion study, bile samples were collected periodically via bile duct cannulation over 72 hours post-administration. The primary route of excretion was urine (male rats: urine: 79%, feces: 16%; female rats: urine: 68%, feces: 28%). Within 24 hours post-administration, 82% of the radiolabeled material was recovered in males and 66% in females. Less than 0.1% of the administered dose of radiolabeled material was recovered from the air. The excretion half-life of the radiolabeled material in urine and feces was 13 to 16 hours in both sexes. Less than 1% of the administered dose of radiolabeled material was recovered from tissues 7 days after administration. In the bile excretion study, 23% and 20% of the administered radiolabeled material were recovered from bile in males and females, respectively. However, its absorption kinetics could not be directly assessed because urine or fecal samples were not collected simultaneously from these study animals.
Absorption can be achieved through leaves, stems, cotyledons, and germinating seeds.

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Metabolites/Metabolites
At least four Sprague-Dawley rats (half male and half female) were administered 100 mg/kg of CPPU-UL-phenyl-(14)C (radiochemical purity: 99.16%; specific activity: 28.04 mCi/mmol) by gavage, supplemented with unlabeled chlorpyrifos technical (purity: 98.2%). The main metabolite recovered in urine was CPPU sulfate with a substituted benzene ring. This metabolite accounted for 84% and 57% of the administered dose in male and female rat urine, respectively. Other metabolites were also products of benzene ring hydroxylation. Hydroxyl-CPPU was the main metabolite recovered in feces, with males and females recovering 11% and 18% of the administered dose, respectively.

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Biological Half-Life
At least four Sprague-Dawley rats (half male and half female) were administered 100 mg/kg of CPPU-UL-phenyl-(14)C (radiochemical purity: 99.16%; specific activity: 28.04 mCi/mmol) by gavage, supplemented with unlabeled chlorpyrifos technical (purity: 98.2%). The excretory half-life in urine and feces was 13 to 16 hours in both male and female rats.

[1]. Identification, synthesis, and safety assessment of forchlorfenuron (1-(2-chloro-4-pyridyl)-3-phenylurea) and its metabolites in kiwifruits. J Agric Food Chem. 2015 Mar 25;63(11):3059-66.

[2]. Dissipation and residue of forchlorfenuron in citrus fruits. Bull Environ Contam Toxicol. 2013 Jun;90(6):756-60.

Chlorpyrifos belongs to the phenylurea class of compounds. Its structure is a urea group, with phenyl and 2-chloropyridin-4-yl groups substituted at positions 1 and 3, respectively. It is a widely used plant growth regulator in agriculture to improve fruit quality and increase fruit size. It is a diphenylurea derivative, belonging to the cytokinin class of growth stimulants, used as a plant growth regulator (PGR) to promote fruit set, increase fruit size, and improve yield. It can be absorbed by most plant tissues and works synergistically with natural auxins to promote cell division and growth. In the United States, it has been approved for use in kiwifruit and grapes, but in China, it has been linked to watermelon bursting incidents. Chlorpyrifos is commonly used in horticulture to promote the growth of kiwifruit and grapes.

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Mechanism of Action
Septin is a filamentous GTPase associated with the cell membrane and cytoskeleton, playing a crucial role in cell division and cell morphogenesis. Septin is associated with various human diseases, including cancer and neuropathy. Small molecules capable of reversibly disrupting septin organization and function will be valuable tools for elucidating septin function and could be used to treat septin-related diseases. Chlorpyrifos is a plant cytokinin that has previously been shown to disrupt the localization of septa proteins in budding yeast. However, it remains unclear whether chlorpyrifos directly targets septa proteins and whether it affects the organization and function of septa proteins in mammalian cells. In this study, we found that chlorpyrifos altered septa protein assembly in vitro without affecting actin or tubulin polymerization. In living mammalian cells, chlorpyrifos inhibited dynamic changes in septa proteins and induced the assembly of abnormally large septa protein structures. Chlorpyrifos exhibited low cytotoxicity, and these effects were reversible upon chlorpyrifos elution. Notably, chlorpyrifos treatment induced defects in mitosis and cell migration, with a phenotype similar to that induced by small interfering RNA (siRNA)-mediated septa protein depletion. It can promote cell division, differentiation, and development; induce callus budding and control apical dominance; break lateral bud dormancy and promote germination; delay senescence and maintain chlorophyll content in detached leaves; regulate nutrient transport; and promote fruit formation, among other benefits.

C12H10CLN3O

247.68

247.051

68157-60-8

Forchlorfenuron-d5;1398065-87-6

93379

White to off-white solid powder

1.3±0.1 g/cm3

426.5±55.0 °C at 760 mmHg

170-172°C

211.7±31.5 °C

0.0±1.1 mmHg at 25°C

1.629

3.83

2

2

2

17

256

0

GPXLRLUVLMHHIK-UHFFFAOYSA-N

InChI=1S/C12H10ClN3O/c13-11-8-10(6-7-14-11)16-12(17)15-9-4-2-1-3-5-9/h1-8H,(H2,14,15,16,17)

1-(2-chloropyridin-4-yl)-3-phenylurea

CPPU; 4PU30 cpd; Forchlorfenuron

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 : ≥ 100 mg/mL (~403.75 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (10.09 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 25.0 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: ≥ 2.5 mg/mL (10.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (10.09 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 25.0 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.)