| 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-benzenediamine)/, DAPA /(3-chloro-2-(2,6-diamino-3-chloro-alpha,alpha,alpha- trifluoromethyl) pyridine)/, and some related conjugates and hydrolysis products were isolated, identified and characterized from urine, feces and bile of radiolabelled fluazinam-treated rats. Fluazinam was almost completely metabolized by hydroxylation, followed by conjugation. A quantitative sex difference was not observed. In a metabolism study in rats, only 33-40% of the administered dose of radio labeled fluazinam was absorbed. Most of the administered dose was recovered in the feces (>89%). Unabsorbed parent compound represented most of the identified radioactivity in the feces. Excretion via the urine was minor (<4%). Total biliary radioactivity, however, represented 25-34% of the administered dose, indicating considerable enterohepatic circulation. Analysis of chromatograms indicated that numerous metabolites were present in the bile. Metabolism / Metabolites ... Fluazinam was almost completely metabolized /in treated rats/ by hydroxylation, followed by conjugation. A quantitative sex difference was not observed. |
|---|---|
| Toxicity/Toxicokinetics |
Toxicity Data
LC50 (rat) = 463 mg/m3 Non-Human Toxicity Values LD50 Rat oral >5000 mg/kg LD50 Rabbit dermal >2000 mg/kg |
| References | |
| Additional Infomation |
Fluazinam is a member of the class of aminopyridines that is 2-amino-5-(trifluoromethyl)pyridine in which one of the amino hydrogens is replaced by a 3-chloro-2,6-dinitro-4-(trifluoromethyl)phenyl group. A fungicide used to control grey mould, downy mildew and other fungal pathogens. It has a role as an apoptosis inducer, an allergen, a xenobiotic, an environmental contaminant and an antifungal agrochemical. It is a C-nitro compound, a chloropyridine, an aminopyridine, a secondary amino compound, a member of monochlorobenzenes and a member of (trifluoromethyl)benzenes.
Fluazinam is a broad-spectrum fungicide used in agriculture. It is classed as a diarylamine and more specifically an arylaminopyridine. The mode of action involves the compound being an extremely potent uncoupler of oxidative phosphorylation in mitochondria and also having high reactivity with thiols. It is unique amongst uncouplers in displaying broad-spectrum activity against fungi and also very low toxicity to mammals due to it being rapidly metabolised to a compound without uncoupling activity. Fluazinam is a protectant fungicide, but is neither systemic or curative. It acts by inhibiting the germination of spores and the development of infection structures. Although it has activity against many fungi, it is less potent against rusts and powdery mildew and as such has not been commercialised for use in cereal crops. It is widely used to control late blight (P. infestans) in potato due to its activity against the zoospores of the pathogen which makes it particularly effective at controlling infection of the potato tubers. Mechanism of Action Fluazinam is a lipophilic weak acid with strong uncoupling activity on 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
