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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)
Biological Activity for NESS 0327
NESS 0327 is an 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.
Compound Libraries for NESS 0327
NESS 0327 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for NESS 0327
| 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 for NESS 0327
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.8 | 20 |
Preparing Stock Solutions for NESS 0327
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.
| 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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Product Datasheets for NESS 0327
References for NESS 0327
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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Keywords: NESS 0327, NESS 0327 supplier, NESS0327, cannabinoid, receptors, CB1, antagonists, antagonism, ultra, high, affinity, selective, Receptors, 5746, Tocris Bioscience
Citations for NESS 0327
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Literature in this Area
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