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NP118809

Catalog No.
A3666
N-type calcium channel blocker
Grouped product items
SizePriceStock Qty
100mg
$70.00
In stock
200mg
$98.00
In stock
500mg
$120.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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:

Chemical Properties

StorageStore at -20°C
M.Wt460.61
Cas No.41332-24-5
FormulaC32H32N2O
Synonyms39-1B4;NP 118809;NP-118809
Solubilityinsoluble in H2O; insoluble in EtOH; ≥63.4 mg/mL in DMSO
Chemical Name1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one
SDFDownload SDF
Canonical SMILESC1CN(CCN1C(C2=CC=CC=C2)C3=CC=CC=C3)C(=O)CC(C4=CC=CC=C4)C5=CC=CC=C5
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

NP118809