A potent CB1 receptor antagonist
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NESS 0327

Item No. 10004184

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydro-N-1-piperidinyl-benzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide
CAS Number
494844-07-4
Molecular Formula
C24H23Cl3N4O
Formula Weight
489.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.5 mg/mlDMSO: 0.25 mg/mlEthanol: 0.25 mg/ml
SMILES
Clc1ccc2c(CCCc3c(nn(c23)c2ccc(Cl)cc2Cl)C(=O)NN2CCCCC2)c1
InChi Code
InChI=1S/C24H23Cl3N4O/c25-16-7-9-18-15(13-16)5-4-6-19-22(24(32)29-30-11-2-1-3-12-30)28-31(23(18)19)21-10-8-17(26)14-20(21)27/h7-10,13-14H,1-6,11-12H2,(H,29,32)
InChi Key
NCXBPZJQQSNIRA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $30

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    5 mg

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    10 mg

    $238

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    50 mg

    $891

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    Product Description

    NESS 0327 is an extremely potent cannabinoid (CB) receptor antagonist with high selectivity for the CB1 receptor compared to the CB2 receptor with Ki values of 0.35 pM and 21 nM, respectively.1 It is a much more potent antagonist and more selective for the CB1 receptor compared to SR 141716A (rimonabant). At nM concentrations NESS 0327 competitively inhibits the binding of the synthetic CB agonist WIN 55,212-2 in isolated rat cerebella membranes and murine vas deferens.1,2 Unlike SR 141716A, NESS 0327 at higher doses does not act as a CB1 receptor inverse agonist and does not produce any physiological effects of its own.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ruiu, S., Pinna, G.A., Marchese, G., et al. Synthesis and characterization of NESS 0327: A novel putative antagonist of the CB1 cannabinoid receptor. J. Pharmacol. Exp. Ther. 306(1), 363-370 (2003).

    2. Tambaro, S., Mongeau, R., Dessi, C., et al. Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors. Eur. J. Pharmacol. 525(1-3), 150-153 (2005).