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NP118809,N 型钙通道 (N-type calcium channel) 阻滞剂

NP118809 （订货以英文为准）

编号：N125978
CAS号：41332-24-5
分子式：C32H32N2O
分子量：460.61
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N125978-10mg 阿拉丁 10mg ¥73.90
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N125978-50mg 阿拉丁 50mg ¥259.90
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N125978-5mg 阿拉丁 5mg ¥45.90
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N125978-250mg 阿拉丁 250mg ¥584.90
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N125978-100mg 阿拉丁 100mg ¥340.90
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N125978-25mg 阿拉丁 25mg ¥174.90
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N125978-1g 阿拉丁 1g ¥1834.90
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N125978-500mg 阿拉丁 500mg ¥1044.90
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产品名称 NP118809
中文名称 NP118809,N 型钙通道 (N-type calcium channel) 阻滞剂
CAS号 41332-24-5
分子式（M.F.） C32H32N2O
分子量（M.W.） 460.61
储存条件 -20°C储存
溶解性25°C: DMSO
存贮条件储存温度-20°C
生化机理Description:IC50 Value: 0.11uM (for N-type Calcium channel) [1]NP-118809 is a potent N-type calcium channel blockers which have good selectivity over L-type calcium channels.in vitro: NP-118809, exhibited increased N-type channel blockade (IC50=0.11 uM) and was 111-fold more selective for N-type channels (L-type calcium channel IC50=12.2 uM) [1]. In the N,4-dibenzhydryl-piperazine-1-carboxamide series (21-27), non-substituted derivative (21) showed a similar inhibitory activity for N-type calcium channels (est. IC50=0.15 uM) as that of parent compound, NP-118809 (est. IC50=0.11 uM). 1-[Phenyl(pyridin-4-yl)methyl]piperazine (42), with no substituent on the nitrogen showed good N-type blocking activity (est. IC50=0.06 uM) while the N-methylated analog (43) was an order of magnitude less potent (est. IC50=0.69 uM) [2].in vivo: NP-118809, i.v. at 2 mg/kg or p.o. at 10 mg/kg in rats, showed acceptable absorption (Tmax=2.3 hr) and half-life (2.1 hr) characteristics and a mean oral bioavailability of 30%. Both compounds were widely distributed outside of plasma and/or bound to plasma proteins. Upon i.p. administration of NP-118809 and NP-078585 at 25 mg/kg, both showed analgesic activity in Phase IIA portions of the rat formalin model. A single 1 uM dose application of NP-078585 blocked hERG currents showing its potential for cardiovascular liability [1].Clinical trial:
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