PZ0386

PF-06456384 trihydrochloride

≥98% (HPLC)

• Synonym(s): 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)
• Empirical Formula (Hill Notation): C₃₅H₃₂F₃N₇O₃S₂ · 3HCl
• CAS Number: 1834610-75-1
• Molecular Weight: 829.18
• UNSPSC Code: 12352202
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: H₂O: 2 mg/mL, clear
• storage temp.: 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

Description

Biochem/physiol Actions

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).

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable