产品说明
生化/生理作用
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).
法律信息
Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.
基本信息
经验(实验)分子式 | C24H32N2O |
分子量 | 364.52 |
MDL编号 | MFCD14635427 |
NACRES | NA.77 |
产品性质
测定 | ≥98% (HPLC) |
形式 | powder |
manufacturer/tradename | Pfizer® |
颜色 | white to beige |
溶解性 | DMSO: 2 mg/mL, clear (warmed) |
创始人 | Pfizer |
储存温度 | room temp |
SMILES string | CC1CCCC(C)N1CCCNC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O |
InChI | 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) |
InChI key | QNZVKSNHNMBPSR-UHFFFAOYSA-N |
安全信息
象形图 | |
警示用语: | Warning |
危险声明 | H302 |
预防措施声明 | P301 + P312 + P330 |
危险分类 | Acute Tox. 4 Oral |
储存分类代码 | 13 - Non Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |