NP118809

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Chemical Structure| 41332-24-5 同义名 : 39-1B4
CAS号 : 41332-24-5
货号 : A254092
分子式 : C32H32N2O
纯度 : 98%
分子量 : 460.609
MDL号 : MFCD03387795
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(108.55 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Calcium Channel

    L-type calcium channel, IC50:12.2 μM

    N-type Ca2+ channel, IC50:0.11 μM
描述 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[3]. 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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.86mL

2.17mL

1.09mL

21.71mL

4.34mL

2.17mL
参考文献

[1]Pajouhesh H, Feng ZP, et al. Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1378-83.

[2]Zamponi GW, Feng ZP, 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.

[3]Zamponi GW, Feng ZP, Zhang L, et al. Scaffold-based design and synthesis of potent N-type calcium channel blockers. Bioorg Med Chem Lett. 2009;19(22):6467‐6472