Basic Info

Common NameAmitraz(F05680)
2D Structure
FRCD IDF05680
CAS Number33089-61-1
PubChem CID36324
FormulaC19H23N3
IUPAC Name

N'-(2,4-dimethylphenyl)-N-[(2,4-dimethylphenyl)iminomethyl]-N-methylmethanimidamide

InChI Key

QXAITBQSYVNQDR-UHFFFAOYSA-N

InChI

InChI=1S/C19H23N3/c1-14-6-8-18(16(3)10-14)20-12-22(5)13-21-19-9-7-15(2)11-17(19)4/h6-13H,1-5H3

Canonical SMILES

CC1=CC(=C(C=C1)N=CN(C)C=NC2=C(C=C(C=C2)C)C)C

Isomeric SMILES

CC1=CC(=C(C=C1)N=CN(C)C=NC2=C(C=C(C=C2)C)C)C

Synonyms
        
            Triazid
        
            BAAM
        
            AMITRAZ
        
            33089-61-1
        
            Mitac
        
            Taktic
        
            Azaform
        
            Mitaban
        
            Acarac
        
            Azadieno
        
Classifies
                

                  
                    Illegal Additives
                  
                    Pesticide
                  

                
        
Update DateNov 13, 2018 17:07

Chemical Taxonomy

KingdomOrganic compounds
SuperclassBenzenoids
ClassBenzene and substituted derivatives
SubclassXylenes
Intermediate Tree NodesNot available
Direct Parentm-Xylenes
Alternative Parents
Molecular FrameworkAromatic homomonocyclic compounds
SubstituentsM-xylene - Formamidine - Organic 1,3-dipolar compound - Propargyl-type 1,3-dipolar organic compound - Carboxylic acid amidine - Amidine - Organic nitrogen compound - Organopnictogen compound - Hydrocarbon derivative - Organonitrogen compound - Aromatic homomonocyclic compound
DescriptionThis compound belongs to the class of organic compounds known as m-xylenes. These are aromatic compounds that contain a m-xylene moiety, which is a monocyclic benzene carrying exactly two methyl groups at the 1- and 3-positions.

Properties

Property NameProperty Value
Molecular Weight293.414
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count2
Rotatable Bond Count4
Complexity354
Monoisotopic Mass293.189
Exact Mass293.189
XLogP5.5
Formal Charge0
Heavy Atom Count22
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Isotope Atom Count0
Covalently-Bonded Unit Count1

ADMET

Model Result Probability
Absorption
Blood-Brain BarrierBBB+0.8995
Human Intestinal AbsorptionHIA+0.7645
Caco-2 PermeabilityCaco2+0.7328
P-glycoprotein SubstrateNon-substrate0.7867
P-glycoprotein InhibitorNon-inhibitor0.6648
Non-inhibitor0.6497
Renal Organic Cation TransporterNon-inhibitor0.5691
Distribution
Subcellular localizationMitochondria0.7465
Metabolism
CYP450 2C9 SubstrateNon-substrate0.6259
CYP450 2D6 SubstrateNon-substrate0.7055
CYP450 3A4 SubstrateNon-substrate0.5134
CYP450 1A2 InhibitorNon-inhibitor0.5242
CYP450 2C9 InhibitorNon-inhibitor0.7996
CYP450 2D6 InhibitorNon-inhibitor0.5735
CYP450 2C19 InhibitorInhibitor0.5505
CYP450 3A4 InhibitorNon-inhibitor0.8309
CYP Inhibitory PromiscuityHigh CYP Inhibitory Promiscuity0.8974
Excretion
Toxicity
Human Ether-a-go-go-Related Gene InhibitionWeak inhibitor0.9705
Non-inhibitor0.7973
AMES ToxicityNon AMES toxic0.9132
CarcinogensCarcinogens 0.6526
Fish ToxicityHigh FHMT0.8057
Tetrahymena Pyriformis ToxicityHigh TPT0.8939
Honey Bee ToxicityLow HBT0.8350
BiodegradationNot ready biodegradable1.0000
Acute Oral ToxicityII0.7578
Carcinogenicity (Three-class)Warning0.4488

Model Value Unit
Absorption
Aqueous solubility-5.4073LogS
Caco-2 Permeability1.6879LogPapp, cm/s
Distribution
Metabolism
Excretion
Toxicity
Rat Acute Toxicity2.8358LD50, mol/kg
Fish Toxicity1.2096pLC50, mg/L
Tetrahymena Pyriformis Toxicity1.3948pIGC50, ug/L

MRLs

FoodProduct CodeCountryMRLsApplication DateNotes
YamJapan0.05ppm
OnionJapan0.05ppm
Aril spices0870000European Union0.1*26/04/2017
Other Terrestrial Mammals,Edible OffalJapan0.2ppm
Pig,Edible OffalJapan0.2ppm
Cattle,Edible OffalJapan0.2ppm
Other Terrestrial Mammals,KidneyJapan0.2ppm
Pig,KidneyJapan0.2ppm
Cattle,KidneyJapan0.2ppm
Other Terrestrial Mammals,LiverJapan0.2ppm
Pig,LiverJapan0.2ppm
Cattle,LiverJapan0.2ppm
Other Terrestrial Mammals,FatJapan0.4ppm
Pig,FatJapan0.1ppm
Cattle,FatJapan0.1ppm
Other Terrestrial Mammals,MuscleJapan0.1ppm
Pig,MuscleJapan0.05ppm
Cattle,MuscleJapan0.05ppm
Other HerbsJapan0.05ppm
Other SpicesJapan0.5ppm

References

TitleJournalDatePubmed ID
Chemical tick control practices in southwestern and northwestern Uganda.Ticks Tick Borne Dis2018 May29606621
Acaricide, fungicide and drug interactions in honey bees (Apis mellifera).PLoS One201323382869
Laboratory evaluation of verbutin as a synergist of acaricides against larvae of Rhipicephalus (Boophilus) microplus (Acari: Ixodidae).J Econ Entomol2010 Aug20857748
Desorption electrospray ionization mass spectrometry for trace analysis of agrochemicals in food.Anal Chem2009 Jan 1519090743
Evaluation of developmental toxicity of amitraz in Sprague-Dawley rats.Arch Environ Contam Toxicol2007 Jan17083001

Targets

General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol.
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen. Participates in the bioactivation of carcinogenic aromatic and heterocyclic amines. Catalizes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin.
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Cytokine activity
Specific Function:
Produced by activated macrophages, IL-1 stimulates thymocyte proliferation by inducing IL-2 release, B-cell maturation and proliferation, and fibroblast growth factor activity. IL-1 proteins are involved in the inflammatory response, being identified as endogenous pyrogens, and are reported to stimulate the release of prostaglandin and collagenase from synovial cells.
Gene Name:
IL1A
Uniprot ID:
P01583
Molecular Weight:
30606.29 Da
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Urokinase plasminogen activator receptor activity
Specific Function:
Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation effects of U-PA. It is subject to negative-feedback regulation by U-PA which cleaves it into an inactive form.
Gene Name:
PLAUR
Uniprot ID:
Q03405
Molecular Weight:
36977.62 Da
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
Gene Name:
CCL2
Uniprot ID:
P13500
Molecular Weight:
11024.87 Da
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]