NP118809 |
| رقم الكتالوجGC36766 |
NP118809 هو مانع قوي لقنوات الكالسيوم من النوع N ، مع IC50 من 0.11 ميكرومتر ؛ يثبط أيضًا بشكل أقل فعالية قناة الكالسيوم من النوع L مع IC بمقدار 12.2 ميكرومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 41332-24-5
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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