NP-118809|NP118809|N-type calcium channel blocke

Cas No.:	41332-24-5
Chemical Name:	1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one
Synonyms:	NP 118809,NP118809
SMILES:	O=C(N1CCN(C(C2=CC=CC=C2)C3=CC=CC=C3)CC1)CC(C4=CC=CC=C4)C5=CC=CC=C5
Formula:	C₃₂H₃₂N₂O
M.Wt:	460.62
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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.
Target:	N-Type Ca2+ Channel:0.11 μM (IC50) L-type calcium channel:12.2 μM (IC50)
In Vivo:	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].
In Vitro:	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].
References:	[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.

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