A-967079

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A-967079__TRPA1 blocker GSK126

Product Name A-967079
Description

TRPA1 blocker
Purity >98%
CAS No. 1170613-55-4
Molecular Formula C12H14FNO
Molecular Weight 207.3
Storage Temperature -20ºC
Shipping Temperature Shipped Ambient
Product Type Inhibitor
Solubility Soluble in DMSO (25 mg/ml)
Source Synthetic
Appearance White solid
SMILES CC/C(=NO)/C(=C/C1=CC=C(C=C1)F)/C
InChI InChI=1S/C12H14FNO/c1-3-12(14-15)9(2)8-10-4-6-11(13)7-5-10/h4-8,15H,3H2,1-2H3/b9-8+,14-12+
InChIKey HKROEBDHHKMNBZ-CHBKHGQFSA-N
Safety Phrases Classification: Caution: Substance not yet fully tested.
Safety Phrases:
S22 – Do not breathe dust
S24/25 – Avoid contact with skin and eyes
S36/37/39 – Wear suitable protective clothing, gloves and eye/face protection
Hazard Phrases:
H302-H315-H317-H318-H335
Precautionary Phrases:
P261-P280-P305 + P351 + P338
Cite This Product A-967079 (StressMarq Biosciences Inc., Victoria BC CANADA, Catalog # SIH-301)

References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19111245

Alternative Names (1E,3E)-1-(4-Fluorophenyl)-N-hydroxy-2-methyl-1-penten-3-imine
Research Areas Ion Channels, Neuroscience, Transient Receptor Potential Channels
PubChem ID 42641861
Scientific Background A-967079 is a TRPA1 antagonist (1) and cell permeable. It has been found to be a potent blocker of TRPA1 channels. It is an oxime analogue and resembles AP18 from a structural perspective, although it has a methyl addition and a chlorine–fluorine substitution. However, compared with AP18 and HC-030031, A-967079 is significantly more potent (100-fold on human and 24-fold on rat TRPA1) and has a much improved pharmacokinetic profile. A-967079 is also more selective, with >1000-fold selectivity over other TRP channels and >150-fold selectivity over 75 other tested proteins (2).
References 1. McGaraughty S., et al. (2010) Mol Pain. 6: 14. 2. Chen et al. (2011) PAIN. 152: 1165–1172.

A-967079

Posted by

A-967079__TRPA1 blocker GSK126

Product Name A-967079
Description

TRPA1 blocker
Purity >98%
CAS No. 1170613-55-4
Molecular Formula C12H14FNO
Molecular Weight 207.3
Storage Temperature -20ºC
Shipping Temperature Shipped Ambient
Product Type Inhibitor
Solubility Soluble in DMSO (25 mg/ml)
Source Synthetic
Appearance White solid
SMILES CC/C(=NO)/C(=C/C1=CC=C(C=C1)F)/C
InChI InChI=1S/C12H14FNO/c1-3-12(14-15)9(2)8-10-4-6-11(13)7-5-10/h4-8,15H,3H2,1-2H3/b9-8+,14-12+
InChIKey HKROEBDHHKMNBZ-CHBKHGQFSA-N
Safety Phrases Classification: Caution: Substance not yet fully tested.
Safety Phrases:
S22 – Do not breathe dust
S24/25 – Avoid contact with skin and eyes
S36/37/39 – Wear suitable protective clothing, gloves and eye/face protection
Hazard Phrases:
H302-H315-H317-H318-H335
Precautionary Phrases:
P261-P280-P305 + P351 + P338
Cite This Product A-967079 (StressMarq Biosciences Inc., Victoria BC CANADA, Catalog # SIH-301)

References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19111245

Alternative Names (1E,3E)-1-(4-Fluorophenyl)-N-hydroxy-2-methyl-1-penten-3-imine
Research Areas Ion Channels, Neuroscience, Transient Receptor Potential Channels
PubChem ID 42641861
Scientific Background A-967079 is a TRPA1 antagonist (1) and cell permeable. It has been found to be a potent blocker of TRPA1 channels. It is an oxime analogue and resembles AP18 from a structural perspective, although it has a methyl addition and a chlorine–fluorine substitution. However, compared with AP18 and HC-030031, A-967079 is significantly more potent (100-fold on human and 24-fold on rat TRPA1) and has a much improved pharmacokinetic profile. A-967079 is also more selective, with >1000-fold selectivity over other TRP channels and >150-fold selectivity over 75 other tested proteins (2).
References 1. McGaraughty S., et al. (2010) Mol Pain. 6: 14. 2. Chen et al. (2011) PAIN. 152: 1165–1172.