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Safety Information

PZ0386

Sigma-Aldrich

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)

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About This Item

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

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

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).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

PDSCL

Deleterious substance

JAN Code

PZ0386-VAR:
PZ0386-BULK:
PZ0386-25MG:
PZ0386-5MG:

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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R Ian Storer et al.
Bioorganic & medicinal chemistry letters, 27(21), 4805-4811 (2017-10-17)
The discovery and selection of a highly potent and selective Na

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