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NESS 0327 (CAS 494844-07-4) LS-H2

CB1 antagonist
LS-H2-1 / 1 mg / $285
LS-H2-5 / 5 mg / $830
LS-H2-10 / 10 mg / $1455
USA Shipment Only
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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. 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. 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. H2_ChemicalStructureImage.png
8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydro-N-1-piperidinyl-benzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide
 
biochemical, chemical, antagonist
LS-H2
494844-07-4
C24H23Cl3N4O
≥98%
A crystalline solid
0
Clc1ccc2c(CCCc3c(nn(c23)c2ccc(Cl)cc2Cl)C(=O)NN2CCCCC2)c1
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)
NCXBPZJQQSNIRA-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 year shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: CNR1 / CB1 related products

Usage Information

NESS 0327 is supplied as a crystalline solid. A stock solution may be made by dissolving the NESS 0327 in an organic solvent purged with an inert gas. NESS 0327 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of NESS 0327 in ethanol and DMSO is approximately 0.25 mg/ml and approximately 0.5 mg/ml in DMF. If aqueous stock solutions are required for biological experiments, they can best be prepared by diluting the organic solvent into aqueous buffers or isotonic saline. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. We do not recommend storing the aqueous solution for more than one day.

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, 150-153 (2005).

 


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