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Description: High affinity and selective CB1 antagonist
Chemical Name: 3-(4-Chlorophenyl)-N-[(4-Chlorophenyl)sulfonyl]-4,5-dihydro-N'-methyl-4-phenyl-1H-pyrazole-1-carboximidamide
Purity: ≥98% (HPLC)
Biological Activity
High affinity and selective CB1 receptor antagonist (Ki = 7.8 nM). Exhibits 1000-fold selectivity for CB1 over CB2 receptors. Inhibits CP 55,940-induced hypotension and WIN 55,212-2-induced hypothermia in vivo. Orally active.
Technical Data
| M. Wt | 487.4 |
| Formula | C23H20Cl2N4O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 362519-49-1 |
| PubChem ID | 11179267 |
| InChI Key | AXJQVVLKUYCICH-UHFFFAOYSA-N |
| Smiles | ClC(C=C4)=CC=C4C1=NN(/C(NS(C3=CC=C(Cl)C=C3)(=O)=O)=N\C)CC1C2=CC=CC=C2 |
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 | 48.74 | 100 | |
| ethanol | 4.87 | 10 with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 487.4. 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 |
|---|---|---|---|
| 1 mM | 2.05 mL | 10.26 mL | 20.52 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.1 mL |
| 10 mM | 0.21 mL | 1.03 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.41 mL |
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References
References are publications that support the biological activity of the product.
Lange et al (2004) Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB1 cannabinoid receptor antagonists. J.Med.Chem. 47 627 PMID: 14736243
Lange et al (2005) Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. Bioorg.Med.Chem.Lett. 15 4794 PMID: 16140010
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