For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>NP-118809(39-1B4) is a potent N-type calcium channel blockers(IC50= 0.11 uM) ; good selectivity over L-type calcium channels.<br>IC50 Value: 0.11 uM (for N-type Calcium channel) [1]<br>Target: N-type calcium channel<br>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].<br>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].</p>
| Catalog Number | I003499 |
| CAS Number | 41332-24-5 |
| Synonyms | 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one |
| Molecular Formula | C32H32N2O |
| Purity | ≥95% |
| Target | Calcium Channel |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IC50 | 0.11 uM (for N-type Calcium channel) [1] |
| Reference | <p style=/line-height:25px/> |
