NP118809-39-1B4-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENP118809Cat. No.: HY-14462CAS No.: 41332-24-5Synonyms: 39-1B4分式: CHNO分量: 460.61作靶点: Calcium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解

2、性数据体外实验 DMSO : 50 mg/mL (108.55 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.43 mM); Suspended solution; Need ultrasonic and warming2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.43 mM); Clear solution1/2 Master of Small Molecules 您边的

3、抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.43 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 NP118809种有效的 N 型钙通道 (N-type calcium channel) 阻滞剂，IC50 值为 0.11 M；同时可较弱地抑制 L 型钙通道 (L-type calcium channel)，IC50 值为 12.2 M。IC50 & Target N-Type Ca2+ Channel L-type calcium channel0.1

4、1 M (IC50) 12.2 M (IC50)体外研究 NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 M; also inhibits L-type calciumchannel with an IC50 of 12.2 M. NP118809 inhibits the hERG potassium channel in HEK cells, with an IC50of 7.4 M 1.体内研究 NP118809 (25 mg/kg, i.p.) shows significant ana

5、lgesic activity in the phase IIA portions of the rat formalinmodel 1. NP118809 (30 mg/kg, p.o.) results in 80.3% inhibition of mechanical allodynia and 96.3% inhibitionof thermal hyperalgesia in the rat spinal nerve ligation model 2.REFERENCES1. Zamponi GW, et al. Scaffold-based design and synthesis

6、 of potent N-type calcium channel blockers. Bioorg Med Chem Lett. 2009 Nov15;19(22):6467-72.2. Pajouhesh H, et al. Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorg Med Chem Lett. 2010Feb 15;20(4):1378-83.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-