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NESS-0327

Chemical Structure : NESS-0327

CAS No.: 494844-07-4

NESS-0327 (NESS 0327;NESS0327)

Catalog No.: PC-60757Not For Human Use, Lab Use Only.

NESS-0327 (NESS0327) is a potent, selective CB1 cannabinoid receptor antagonist with Ki of 350 fM, >60,000-fold selective for the CB1 receptor versus CB2 receptor (Ki=21 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

NESS-0327 (NESS0327) is a potent, selective CB1 cannabinoid receptor antagonist with Ki of 350 fM, >60,000-fold selective for the CB1 receptor versus CB2 receptor (Ki=21 nM).
NESS-0327 antagonizes WIN 55,212-2-stimulated [35S]GTPgammaS binding, antagonizes the inhibitory effects of WIN 55,212-2 on electrically evoked contractions in mouse isolated vas deferens preparations with pA2 12.46.
NESS-0327 inhibits the antinociceptive effect produced by WIN 55,212-2 (2 mg/kg s.c.) in both tail-flick (ID50=0.042 mg/kg i.p.) and hot-plate test (ID50=0.018 mg/kg i.p.).

Physicochemical Properties

M.Wt 489.8
Formula C24H23Cl3N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-piperidinyl-[8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydrobenzo [6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide

References

1. Ruiu S, et al. J Pharmacol Exp Ther. 2003 Jul;306(1):363-70.

2. Tambaro S, et al. Eur J Pharmacol. 2005 Nov 21;525(1-3):150-3.

3. Murineddu G, et al. J Med Chem. 2005 Nov 17;48(23):7351-62.

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