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NP118809
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NP118809图片
CAS NO:41332-24-5
包装与价格:
包装价格(元)
Free Sample (0.1-0.5mg)电议
10mM (in 1mL DMSO)电议
100mg电议
200mg电议
500mg电议
1g电议
5g电议

产品介绍
NP118809 是一种有效的 N 型钙通道 (N-type calcium channel) 阻滞剂,IC50 值为 0.11 μM;同时可较弱地抑制 L 型钙通道 (L-type calcium channel),IC50 值为 12.2 μM。
Cas No.41332-24-5
别名1-【4-(二苯甲基)-1-哌嗪基】-3,3-二苯基-1-丙酮,39-1B4
Canonical SMILESO=C(CC(C1=CC=CC=C1)C2=CC=CC=C2)N3CCN(C(C4=CC=CC=C4)C5=CC=CC=C5)CC3
分子式C32H32N2O
分子量460.61
溶解度DMSO: 50 mg/mL (108.55 mM); Water:< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also less potently inhibits L-type calcium channel with an IC50 of 12.2 μM. N-Type Ca2+ Channel|0.11 μM (IC50)|L-type calcium channel|12.2 μM (IC50)

NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also inhibits L-type calcium channel with an IC50 of 12.2 μM. NP118809 inhibits the hERG potassium channel in HEK cells, with an IC50 of 7.4 μM[1].

NP118809 (25 mg/kg, i.p.) shows significant analgesic activity in the phase IIA portions of the rat formalin model[1]. NP118809 (30 mg/kg, p.o.) results in 80.3% inhibition of mechanical allodynia and 96.3% inhibition of thermal hyperalgesia in the rat spinal nerve ligation model[2].

[1]. Zamponi GW, et al. Scaffold-based design and synthesis of potent N-type calcium channel blockers. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72. [2]. Pajouhesh H, et al. Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1378-83.