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Chemical Structure : NESS-0327
CAS No.: 494844-07-4
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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|---|---|---|---|
| 5 mg | $498 | In stock | |
| 10 mg | $788 | In stock | |
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| 100 mg | Get quote |
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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.).
| M.Wt | 489.8 | |
| Formula | C24H23Cl3N4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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