TargetMol

AM-0466

Product Code:
 
TAR-T26606
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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Further Information

Bioactivity:
AM-0466 is a potent and selective NaV1.7 Inhibitor (Nav 1.7 IC50 = 21 nM; Nav 1.5 IC50 =>30.0 uM. PXR = 22% @10 uM; CYP 2C9 IC50 = 4.6 uM; CYP3A4 TDI IC50 =>50.0 uM.). AM-0466 Affords Robust in Vivo Activity. AM-0466 demonstrated robust pharmacodynamic activity in a NaV1.7-dependent model of histamine-induced pruritus (itch) and additionally in a capsaicin-induced nociception model of pain without any confounding effect in open-field activity.
CAS:
T26606
Molecular Weight:
552.53
Purity:
0.98
SMILES:
O=S(NC1=NC=CC=N1)(C2=CC=C(N(C3=CC=C(C4=CC=CC=C4C(F)(F)F)C=C3OC)C(C=C5)=O)C5=C2)=O

References

Graceffa RF, Boezio AA, Able J, et al. Sulfonamides as Selective Na(V)1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity. J Med Chem. 2017 Apr 20. doi: 10.1021/acs.jmedchem.6b01850. [Epub ahead of print] PubMed PMID: 28324649.