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PD-85639,≥98% (HPLC)

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

Empirical Formula (Hill Notation): C24H32N2O CAS号: 149838-21-1 分子量: 364.52 MDL编号: MFCD14635427 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): PZ0370
CAS号: 149838-21-1
MDL号: MFCD14635427
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$365.77

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°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).
 
PD-85639 (PD85,639) 是一种电压门控钠 (Na+) 通道阻滞剂(25 μM PD85,639 在 10 分钟内 75% 和在 25 分钟内阻断 Na+ 电流超过 95%;全细胞膜片钳使用初级 大鼠脑神经元),显示以同时具有高亲和力和低亲和力结合模式(EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3)靶向大鼠脑 Nav1.2 μM/72% 在 pH 7.4,针对 2 nM [3H]-PD85,639,用于结合大鼠脑突触体;EC50 = 17 nM/39% & 10 μM/61%,在 pH 9.0 下使用大鼠脑突触体膜)和快速 动力学(4°C 时 t1/2 = 1.2,25°C 时 <0.5 分钟),与局麻药 Na+ 通道阻滞剂丁卡因、布比卡因和甲哌卡因以及 Na+ 通道激活剂藜芦定和烟曲霉毒素(K1 = 0.26 μM)竞争 5 nM [3H]-BTX 用于结合大鼠新生膜)。
 

法律信息

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

属性

测定

≥98% (HPLC)

形式

powder

mfr. no.

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

Exclamation mark

警示用语:

Warning

危险声明

预防措施声明

RIDADR

NONH for all modes of transport

商品规格
属性名称属性值
储存温度 Storage temp.常温阴凉避光
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16