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A-079 | Antagonist of TRPA1
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
TRPA1
  • IC50:67 nM
  • IC50:51 nM
Antagonist
1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
A-967079 is >1000-fold selective over other TRP channels (TRPV1, TRPV3, TRPV4, or TRPM8). Outside ta ...

Potency
Cellular
In Vitro

TRPA1

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.pain.2011.01.049

In Vivo Validations

Rat
Dose: 30 μmol/kg
Route of delivery: Intravenous
Bioavailability: 37% (oral)

DOI Reference: 10.1016/j.pain.2011.01.049

Negative Control Compounds

A-226
Notes: IC50> 100 µM in vitro; shows some off-target activity on SIGMAR1 (Ki=528.8 nM)

Chemical Information

Molecular Formula C12H14FNO
SMILEs CCC(=N\O)/C(C)=C/c1ccc(F)cc1
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+
Molecular weight 207.11 Da
AlogP 0.0
HBond acceptors 2
HBond donors 1
Atoms 29

Vendors

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Expert Reviews

No SERP comments found for A-079

Probe A-079 is in the process of SERP review.

Please continue to check back for new reviews and commentary.