化学性质
| Storage | Store at -20°C |
| M.Wt | 460.61 |
| Cas No. | 41332-24-5 |
| Formula | C32H32N2O |
| Synonyms | 39-1B4;NP 118809;NP-118809 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥63.4 mg/mL in DMSO |
| Chemical Name | 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one |
| Canonical SMILES | C1CN(CCN1C(C2=CC=CC=C2)C3=CC=CC=C3)C(=O)CC(C4=CC=CC=C4)C5=CC=CC=C5 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
资料参考
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:
m.cnreagent.com