PD-85639

C₂₄H₃₂N₂O

364.52

MFCD14635427

NA.77

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℃, <0.5 min at 25℃), 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).

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.

≥98% (HPLC)

powder

Pfizer^®

white to beige

DMSO: 2 mg/mL, clear (warmed)

Pfizer

room temp

CC1CCCC(C)N1CCCNC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O

1S/C23H31N3O/c1-4-13-23(22(24)27,19-9-6-5-7-10-19)20-11-8-12-21(14-20)26-17(2)15-25-16-18(26)3/h5-12,14,17-18,25H,4,13,15-16H2,1-3H3,(H2,24,27)

QNZVKSNHNMBPSR-UHFFFAOYSA-N

GHS07

Warning

H302

P301 + P312 + P330

Acute Tox. 4 Oral

13 - Non Combustible Solids

WGK 3