Absorption, Distribution and Excretion
A rat study of (14)C-formiconazole 50WP showed a systemic absorption rate of 0.27% per hour (6.5% over 24 hours). This calculation was based on a least-squares analysis of 24-hour urinary excretion at dose levels of 49, 460, and 4800 μg/cm² (13.2%, 3.5%, and 1.3%, respectively), and matched to an approximate skin exposure of 2400 μg/cm² based on the 50WP formulation concentration. Formiconazole is rapidly absorbed through the skin, with 95% and 94% of the drug remaining in the skin over 24 hours at dose levels of 4800 and 460 μg/cm², respectively. In the low-dose group, approximately 85% of the administered dose remained in the skin 24 hours after administration. In a comparative study of metabolic fate and biochemical effects, rats and mice received a single oral gavage administration of 14C-labeled formaldehyde. Two hours after administration, most of the radioactive material in the gastrointestinal contents of the high-dose group was present in the stomach as unaltered form of formaldehyde. …At the highest dose, unaltered formaldehyde was present in the cecum of mice, but not detected in the cecum of rats, indicating that this dose was close to the animals' maximum capacity to degrade formaldehyde. Pulsed doses passed through the gastrointestinal tract of mice more rapidly than those of rats. …The radioactive material was rapidly eliminated via all pathways, with most of the 14C dose being eliminated within 24 hours. Oral metabolism studies were conducted in Sprague Dawley rats. Formaldehyde is readily and extensively absorbed and rapidly excreted in the urine. No accumulation of formaldehyde was detected within 5 days post-administration. The main fecal metabolite was phthalimide. Skin absorption studies in rats showed that the absorption rate of formaldehyde was extremely low. The absorption rate of thiram after 72 hours of exposure was 2.7%. For more complete data on the absorption, distribution, and excretion of thiram (7 types), please visit the HSDB record page. Metabolites/Metabolites: In orally administered rodents, thiram has been reported to rapidly degrade into phthalimides and phosgene (via thiocarbonyl chloride). In vitro human blood metabolism studies showed that thiram rapidly degrades into phthalimides with a calculated half-life of 4.9 seconds. Phosgene reacts rapidly with substances such as cysteine or glutathione to detoxify and is ultimately rapidly excreted. …In mammals and birds, thiram undergoes extensive alterations through the combined action of enzymatic and non-enzymatic chemical reactions. Two complementary processes, hydrolysis and thiol interactions, first break down the bactericide into its imide ring and trichloromethyl sulfide complex. Subsequent reactions (some of which may be enzymatic) produce a series of imide degradation products and phosgene-mediated products. These reactions are rapid, with almost all substances excreted from the animals within 24–48 hours; no imides or side chains accumulate. After administration of 14C-benzene-labeled thiram to livestock, most of the radioactive material was excreted in urine and feces. …Analysis of radioactivity in tissue and milk samples revealed the presence of phthalic acid and phthalimides. Ruminant metabolic studies indicated that thiram degradation occurs via the loss of a one-carbon-atom trichloromethyl moiety. This moiety is extensively metabolized, with the radiolabeled carbon atom integrated into thiazolidinyl compounds and natural products. The remaining phenyl-labeled moiety is primarily metabolized to phthalimides and phthalic acid. In a comparative metabolic fate and biochemical effects study, rats and mice were given a single gavage administration of 14C-labeled thiram. ...No degradation of the compound due to the cleavage of the trichloromethyl sulfide side chain (at the ¹⁴C labeling position) was observed in rats or mice. The intestinal contents primarily contained reaction products of phosgene. Metabolites identified in the intestinal contents and intestinal wall included phosgene glutathione conjugates, partially degraded derivatives of these conjugates, thiazolidinyl ether and disulfonic acid. For more complete data on the metabolites/metabolites of FOLPET (7 in total), please visit the HSDB record page.

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Biological half-life
...The calculated half-life is 4.9 seconds.

Toxicity Data
LC50 (Rat) = 480 mg/m³

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Non-human Toxicity Values LC50 Rat Inhalation > 5.0 MG/L/2 HR /Technical/ LC50 Mouse Inhalation > 6.0 MG/L/2 HR /Technical/ LD50 Rabbit (Albino) Dermal > 22,600 mg/kg LC50 Rat Inhalation > 1.89 mg/L/4 hr For more complete non-human toxicity data for FOLPET (8 items), please visit the HSDB records page.

According to an independent committee of scientific and health experts, Folpet may be carcinogenic. Folpet is a white crystalline powder used as a fungicide and is insoluble in water. It belongs to the phthalimide class of compounds, where the hydrogen atom of its nitrogen atom is replaced by a trichloromethyl thio group. As an agricultural fungicide, it has been used since the 1950s to control powdery mildew, leaf spot, and other diseases in crops. It is an antifungal pesticide. It is an organochlorine compound, organosulfur compound, and phthalimide fungicide, functionally related to phthalimide compounds. Folpet is a protective foliar fungicide. Its mechanism of action is to inhibit the normal cell division of various microorganisms. It is used to control cherry leaf spot, rose powdery mildew, rose black spot, and apple scab. It can be used on berries, flowers, ornamental plants, fruits, and vegetables, as well as for seed and seedbed treatment. Folpet is also used as a fungicide in paints and plastics, and as a treatment agent for interior and exterior structural surfaces of buildings. Folpet has low acute toxicity to mammals. It is slightly toxic to birds and bees, and moderately toxic to fish, aquatic invertebrates, algae, and earthworms. Folpet is a strong irritant to the eyes, and repeated or prolonged exposure can cause skin allergies. Chronic exposure studies have shown that Folpet is carcinogenic in mice (but not rats). Based on this, Folpet is considered potentially carcinogenic to humans.

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Mechanism of Action
Both Folpet and captan appear to exert their toxic effects through the reaction of phosgene with the gastrointestinal tract. A more comprehensive review of the mechanism of action of the related fungicide captan has been conducted. Regarding captan, the agency has concluded that phosgene is likely associated with duodenal tumors, although its exact mechanism of action is unclear, and the possibility of genotoxic components cannot be ruled out.

C9H4NO2SCL3

296.55756

294.902

133-07-3

Faltan-d4;1327204-12-5

8607

Crystals from benzene
Light colored powder
Colorless crystals
White crystals

1.7±0.1 g/cm3

333.8±52.0 °C at 760 mmHg

177-180°C

155.7±30.7 °C

0.0±0.7 mmHg at 25°C

1.693

2.85

0

3

1

16

307

0

C1=CC=C2C(=C1)C(=O)N(C2=O)SC(Cl)(Cl)Cl

HKIOYBQGHSTUDB-UHFFFAOYSA-N

InChI=1S/C9H4Cl3NO2S/c10-9(11,12)16-13-7(14)5-3-1-2-4-6(5)8(13)15/h1-4H

2-(trichloromethylsulfanyl)isoindole-1,3-dione

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 : ~125 mg/mL (~421.50 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (7.01 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 20.8 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.)