| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Metabolites AMPA (4-chloro-N2-[3-chloro-5-(trifluoromethyl)-2-pyridyl]-3-nitro-5-(trifluoromethyl)-1,2-phenylenediamine), DAPA (3-chloro-2-(2,6-diamino-3-chloro-α,α,α-trifluoromethyl)pyridine), and some related conjugates and hydrolysis products were isolated, identified, and characterized from the urine, feces, and bile of radiolabeled fluazinam-treated rats. Fluazinam is almost entirely metabolized via hydroxylation followed by conjugation. No sex differences were observed. In rat metabolic studies, only 33–40% of the radiolabeled fluazinam was absorbed. The majority of the administered dose (>89%) was recovered in feces. The radioactive material detected in feces was primarily the unabsorbed parent compound. Very little was excreted in urine (<4%). However, the total radioactive material in bile accounted for 25-34% of the administered dose, indicating significant enterohepatic circulation. Chromatographic analysis revealed the presence of multiple metabolites in the bile. Metabolism/Metabolites …Fluoridamine was almost entirely metabolized in the test rats via hydroxylation, followed by a conjugation reaction. No sex differences were observed. |
|---|---|
| Toxicity/Toxicokinetics |
Toxicity Data
LC50 (Rat) = 463 mg/m³ Non-human Toxicity Values LD50 (Rats, Oral) >5000 mg/kg LD50 (Rabbit, Dermal) >2000 mg/kg |
| References | |
| Additional Infomation |
Fluazinam is an aminopyridine compound, chemically named 2-amino-5-(trifluoromethyl)pyridine, in which one amino hydrogen atom is replaced by 3-chloro-2,6-dinitro-4-(trifluoromethyl)phenyl. It is a fungicide used to control gray mold, downy mildew, and other fungal pathogens. Fluazinam possesses properties such as inducing apoptosis, sensitization, xenobiotic activity, environmental pollution, and antifungal effects. It is a C-nitro compound, a chloropyridine compound, an aminopyridine compound, a secondary amino compound, a monochlorobenzene compound, and a (trifluoromethyl)benzene compound. Fluazinam is a broad-spectrum fungicide widely used in agriculture. It belongs to the diarylamine class of compounds, more specifically, an arylaminopyridine compound. Its mechanism of action lies in its strong uncoupling ability against oxidative phosphorylation in mitochondria and its high reactivity with thiols. Unlike other uncoupling agents, it exhibits broad-spectrum activity against fungi and, due to its rapid metabolism into compounds without uncoupling activity, has extremely low toxicity to mammals. Fluazinam is a protective fungicide, but it is neither systemic nor curative. Its mechanism of action is to inhibit spore germination and the formation of infection structures. Although effective against a variety of fungi, it is less effective against rust and powdery mildew, and therefore has not been commercially used in cereal crops. Due to its activity against the zoospores of pathogens, fluazinam is widely used to control potato late blight (Phytophthora infestans), and is particularly effective in controlling infection of potato tubers.
Mechanism of Action Fluazinam is a lipophilic weak acid with strong uncoupling activity against mitochondria in vitro. |
| Molecular Formula |
C13H4CL2F6N4O4
|
|---|---|
| Molecular Weight |
465.09
|
| Exact Mass |
463.951
|
| CAS # |
79622-59-6
|
| PubChem CID |
91731
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.8±0.1 g/cm3
|
| Boiling Point |
376.1±42.0 °C at 760 mmHg
|
| Melting Point |
113ºC
|
| Flash Point |
181.3±27.9 °C
|
| Vapour Pressure |
0.0±0.9 mmHg at 25°C
|
| Index of Refraction |
1.571
|
| LogP |
8.19
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
29
|
| Complexity |
628
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
UZCGKGPEKUCDTF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H4Cl2F6N4O4/c14-6-1-4(12(16,17)18)3-22-11(6)23-9-7(24(26)27)2-5(13(19,20)21)8(15)10(9)25(28)29/h1-3H,(H,22,23)
|
| Chemical Name |
3-chloro-N-[3-chloro-2,6-dinitro-4-(trifluoromethyl)phenyl]-5-(trifluoromethyl)pyridin-2-amine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~268.77 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.47 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.47 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1501 mL | 10.7506 mL | 21.5012 mL | |
| 5 mM | 0.4300 mL | 2.1501 mL | 4.3002 mL | |
| 10 mM | 0.2150 mL | 1.0751 mL | 2.1501 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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