Merck PF-06456384 trihydrochloride

PF-06456384 trihydrochloride

≥98% (HPLC)

3-Cyano-4-[[3-[2-[[[2-(4-piperidinyl)ethyl]amino]methyl]-4-pyridinyl]-3′-(trifluoromethyl)[1,1′-biphenyl]-4-yl]oxy]-N-1,2,4-thiadiazol-5-yl-benzenesulfonamide trihydrochloride, Benzenesulfonamide, 3-cyano-4-[[3-[2-[[[2-(4-piperidinyl)ethyl]amino]methyl]-4-pyridinyl]-3′-(trifluoromethyl)[1,1′-biphenyl]-4-yl]oxy]-N-1,2,4-thiadiazol-5-yl-, hydrochloride (1:3)

assay

≥98% (HPLC)

form

powder

manufacturer/tradename

Pfizer®

색상

white to beige

solubility

H2O: 2 mg/mL, clear

주관자

Pfizer

저장 온도

room temp

SMILES string

O=S(C(C=C1)=CC(C#N)=C1OC2=C(C3=CC(CNCCC4CCNCC4)=NC=C3)C=C(C5=CC=CC(C(F)(F)F)=C5)C=C2)(NC6=NC=NS6)=O

PF-06456384 is a highly potent and selective inhibitor against voltage-gated sodium channel NaV1.7 (SCN9A; IC50 = 0.01, <0.1, 75 nM against human, mouse, rat Nav1.7, respectively, by conventional patch clamp; human Nav1.7 IC50 = 0.58 nM by PatchExpress electrophysiology) with >300-fold selectivity over other human NaVs (IC50 = 3 nM/NaV1.2, 5.8 nM/NaV1.6, 75 nM/NaV1.7, 314 nM/NaV1.1, 1.45 μM/NaV1.4, 2.59 μM/NaV1.5, 6.44 μM/NaV1.3, 26 μM/NaV1.8).