1642113-59-4

1642113-59-4 structure

Name: AM-0466
Chemical Name: 1-[3-Methoxy-3'-(trifluoromethyl)-4-biphenylyl]-2-oxo-N-(2-pyrimidinyl)-1,2-dihydro-6-quinolinesulfonamide
CAS Number: 1642113-59-4
Molecular Formula: C₂₇H₁₉F₃N₄O₄S
Molecular Weight: 552.524
Create Date: 2020-01-20 03:23:55
Modify Date: 2024-01-06 08:16:27
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.).

Name	1-[3-Methoxy-3'-(trifluoromethyl)-4-biphenylyl]-2-oxo-N-(2-pyrimidinyl)-1,2-dihydro-6-quinolinesulfonamide
Synonyms	1-[3-Methoxy-3'-(trifluoromethyl)-4-biphenylyl]-2-oxo-N-(2-pyrimidinyl)-1,2-dihydro-6-quinolinesulfonamide 6-Quinolinesulfonamide, 1,2-dihydro-1-[3-methoxy-3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-2-oxo-N-2-pyrimidinyl-

Description	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.).
In Vitro	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.