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PZ0370 Sigma-Aldrich

PD-85639

Synonym: N-[3-(2,6-Dimethyl-1-piperidinyl)propyl]-α-phenylbenzeneacetamide, PD 85639, PD85,639, PD85639

  • CAS Number 149838-21-1

  • Empirical Formula (Hill Notation) C24H32N2O

  • Molecular Weight 364.52

  •  MDL number MFCD14635427

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, P-PH
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 2 mg/mL, clear (warmed)
storage temp.   room temp

Description

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

Biochem/physiol Actions

PD-85639 (PD85,639) is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1/2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis

Protocols & Articles
Peer-Reviewed Papers
15

References

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