R&D Systems Inc. Tocris Bioscience Boston Biochem

AM 251

Cat. No. 1117

AM 251 C22H21Cl2IN4O [183232-66-8]

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Chemical Name: N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide

Biological Activity

Potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors. Also potent GPR55 agonist (EC50 = 39 nM). Also available as part of the Cannabinoid CB1 Receptor Tocriset™; and in a fluorescent form (Cat. No. 2540).

Technical Data

M.Wt:
555.24
Formula:
C22H21Cl2IN4O
Solubility:
Soluble to 25 mM in ethanol and to 100 mM in DMSO
Purity:
>99 %
Storage:
Store at RT
CAS No:
183232-66-8

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

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

References

Gatley et al (1996) 125I-labeled AM 251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors. Eur.J.Pharmacol. 307 331. PMID: 8836622.

Gatley et al (1997) Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors. Life Sci. 61 191. PMID: 9335234.

Lan et al (1999) Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J.Med.Chem. 42 769. PMID: 10052983.

Pertwee (2005) Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci. 76 1307. PMID: 15670612.

Ryberg et al (2007) The orphan receptor GPR55 is a novel cannabinoid receptor. Br.J.Pharmacol. 152 1092. PMID: 17876302.

If you know of a relevant citation for this product please let us know.

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Keywords: AM 251, supplier, Potent, CB1, antagonist, GPR55, agonist, cannabinoid, receptors, AM251, cb1r

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