Triforine appears as colorless crystals. Non corrosive. Used as a fungicide.
颜色/状态：
White to light brown crystals.
蒸汽压力：
2.00X10-7 mm Hg at 25 °C.
稳定性/保质期：
对皮肤和眼睛可能引起轻微刺激。
分解：
Decomposed in aqueous solution exposed to u.v. or daylight. Decomposed in strongly acidic media (to trichloroacetaldehyde and piperazine salts) and in strongly alkaline media (to chloroform and piperazine); DT50 (pH 5-7, 25 °C) 3.5 days.
Triforine is rapidly metabolized and excreted in rats; unchanged compound accounts for only 0-5% of the dose. Substantial quantities of unchanged triforine were recovered only from feces. The first metabolite to be identified was N-[2,2,2-trichloro-1-(piperazin-1-yl)ethyl]-formamide, which is formed by the cleavage of an entire side chain. In later metabolic studies with 14C labelling in the piperazine ring and aliphatic side chain, triforine underwent virtually complete metabolism after administration as a single oral dose of 10 mg/kg bw. N-[2,2,2-Trichloro-1-(piperazin-1-yl)ethyl]formamide, the major radiolabelled urinary component in rats receiving [piperazine 14C]-triforine, accounted for 46-53% of the dose over 0-24 hr; however, in rats receiving side-chain-labelled 14C-triforine, the proportion was reduced to 24-27% after a single 10 mg/kg bw dose and 21-24% after repeated doses. It was excreted as the glucuronide. The side-chain metabolite trichloroethanol and its glucuronide represented 18-21% of the dose. Another side-chain metabolite occurring in the urine was the N-acetylcysteine conjugate of 2,2,2-trichloroethylamine, which represented 13-15% of the administered dose. In feces collected from female rats over 0-48 hr, 3.6% of the single 10 mg/kg bw dose and 3.4% of the repeated doses was present as N-[2,2,2-trichloro-1-(piperazin-1-yl)ethyl]formamide. This metabolite was not detected in the feces of rats receiving 1,000 mg/kg bw. Very little unchanged triforine (0-1%) was detected in the feces of rats given the low dose, whereas it represented 70-80% of the dose in rats given 1,000 mg/kg bw. This result suggests that absorption of triforine is a saturable process, unless there is extensive biliary excretion at the high dose.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类：有致癌性的提示性证据，但不足以评估对人类致癌的可能性；可能对人类具有致癌性。
Cancer Classification: Suggestive Evidence of Carcinogenicity, but Not Sufficient to Assess Human Carcinogenic Potential; Likely to be Carcinogenic to Humans
来源:Hazardous Substances Data Bank (HSDB)
毒理性
副作用
皮肤致敏剂 - 一种可以诱导皮肤产生过敏反应的制剂。
Skin Sensitizer - An agent that can induce an allergic reaction in the skin.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
毒性数据
大鼠LC50 > 5120毫克/立方米
LC50 (rat) > 5,120 mg/m3
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
Groups of 25 or 50 male and 25 or 50 female Swiss mice were given 0.05% sodium nitrate in drinking-water, triforine suspended in water at 300 mg/kg bw by gavage twice each week, or a combination of the two treatments for up to 180 days. Tumor incidences were compared with those in a control group of 184 males and 117 females. Triforine alone did not increase the number of tumors; however, the combination increased the frequencies of lymphomas (including thymoma) and of epithelial adenomas and carcinomas of the gastrointestinal tract, the lung, and, in males, the liver. Incubation of triforine with 4% acidified sodium nitrite solution for 24 hr formed dinitrosopiperazine, which is known to be carcinogenic and was suspected to be the substance that induced the tumors.
Skin decontamination. Dermal contamination should be washed off with soap and water. Flush contamination from the eyes with copious amounts of water. If irritation persists, specialized medical care should be obtained. /Miscellaneous organic fungicides/
The absorption and disposition of 14C-triforine suspended in 5% aqueous sodium carboxymethylcellulose was studied in male and female CD Sprague-Dawley-derived rats at doses of 10 mg/kg bw, /orally/ as a single dose and after treatment with unlabelled triforine for 14 days, and 1,000 mg/kg bw as a single radiolabelled dose. Both side-chain and ring-labelled 14C-triforine were available, but piperazine ring-labelled 14C-triforine was used only in a pilot experiment in which a single dose of 10 mg/kg bw was administered to two male and two female rats. In this experiment, the mean proportions of the administered dose excreted during 120 hr were: urine, 77% in males and 82% in females; feces, 18% in males and 19% in females; expired air, 3.3% in males and 1.5% in females; <3% remained in the carcass. Most of the radiolabel (73% in males and 76% in females) was excreted in the urine within 0-24 hr. In the main study with side-chain-labelled 14C-triforine, in which single doses of 10 mg/kg bw were given to five male and five female rats, the mean proportions of the administered dose excreted during 120 hr were: urine, 78% in males and 79% in females; feces, 12% in males and 14% in females; expired air, 5.2% in males and 6.0% in females. Less than 3% remained in the carcass. Most of the radiolabel (75% in males and females) was excreted in the urine within 0-24 hr.
...Side-chain-labelled 14C-triforine was administered /orally/ as a single dose of 1,000 mg/kg bw. The mean proportions of the administered dose excreted during 120 hr were: urine, 11% in males and 19% in females; feces, 85% in males and 77% in females; expired air, 0.9% in males and 1.6% in females. Only about 0.5% remained in the carcass. Most of the urinary radiolabel (7.7% in males and 12% in females) was excreted within 6-48 hr. The delayed urinary excretion (in comparison with /other/ experiments) probably reflects absorption limited by the dissolution rate. More than 90% of the radiolabel recovered from the feces over 0-72 hr was associated with side-chain-labelled 14C-triforine and presumably represented unabsorbed material.
[EN] ACC INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE L'ACC ET UTILISATIONS ASSOCIÉES
申请人：GILEAD APOLLO LLC
公开号：WO2017075056A1
公开（公告）日：2017-05-04
The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
[EN] BICYCLYL-SUBSTITUTED ISOTHIAZOLINE COMPOUNDS<br/>[FR] COMPOSÉS ISOTHIAZOLINE SUBSTITUÉS PAR UN BICYCLYLE
申请人：BASF SE
公开号：WO2014206910A1
公开（公告）日：2014-12-31
The present invention relates to bicyclyl-substituted isothiazoline compounds of formula (I) wherein the variables are as defined in the claims and description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
The present invention relates to azoline compounds of formula (I) wherein A, B1, B2, B3, G1, G2, X1, R1, R3a, R3b, Rg1 and Rg2 are as defined in the claims and the description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
[EN] SUBSTITUTED QUINAZOLINES AS FUNGICIDES<br/>[FR] QUINAZOLINES SUBSTITUÉES, UTILISÉES EN TANT QUE FONGICIDES
申请人：SYNGENTA PARTICIPATIONS AG
公开号：WO2010136475A1
公开（公告）日：2010-12-02
The present invention relates to a compound of formula (I) wherein wherein the substituents have the definitions as defined in claim 1or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.
