PD-85639

• Target :

  Others|||Sodium Channel

• Related Pathways :

  Others|||Membrane transporter/Ion channel

• Bioactivity :

  PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 ?M 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 ?M/60% at pH 9.0, 5 nM/28% & 3 ?M/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 ?M/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 ?M against 5 nM [3H]-BTX for binding rat neocrotical membranes) .

• Smiles :

  C(C(NCCCN1C(C)CCCC1C)=O)(C2=CC=CC=C2)C3=CC=CC=C3

• Molecular Formula :

  C24H32N2O

• Molecular Weight :

  364.52

• Shipping Conditions :

  Cool pack

• Storage Temperature :

  -20°C

• CAS Number :

  149838-21-1