NESS 0327

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Cat.No. 5746 - NESS 0327 | C24H23Cl3N4O | CAS No. 494844-07-4
Description: Ultra-high affinity and selective CB1 antagonist
Chemical 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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (6)

Biological Activity

Ultra-high affinity and selective CB1 receptor antagonist (Ki = 350 fM). Exhibits >60-fold selectivity for CB1 over CB2 receptors. Antagonizes the inhibitory effects of WIN 55,212-2 (Cat. No. 1038) on electrically evoked contractions in mouse isolated vas deferens ex vivo. Also antagonizes the antinociceptive effect of WIN 55,212-2 in tail-flick and hot plate tests in vivo.

Technical Data

M. Wt 489.82
Formula C24H23Cl3N4O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 494844-07-4
PubChem ID 10435654
InChI Key NCXBPZJQQSNIRA-UHFFFAOYSA-N
Smiles O=C(NN1CCCCC1)C2=NN(C3=CC=C(Cl)C=C3Cl)C4=C2CCCC5=C4C=CC(Cl)=C5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 9.8 20

Preparing Stock Solutions

The following data is based on the product molecular weight 489.82. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 10.21 mL 51.04 mL 102.08 mL
1 mM 2.04 mL 10.21 mL 20.42 mL
2 mM 1.02 mL 5.1 mL 10.21 mL
10 mM 0.2 mL 1.02 mL 2.04 mL

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References

References are publications that support the biological activity of the product.

Ruiu et al (2003) Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor. J.Pharmacol.Exp.Ther. 306 363 PMID: 12663689


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Citations for NESS 0327

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