AM 251
Tocris Bioscience | Catalog # 1117
Key Product Details
Description
Product Description
AM 251 is a 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) and μ-opioid receptor antagonist (Ki = 251 nM).
Fluorescent Form also available.
Product Specifications for AM 251
Molecular Weight
Formula
Storage
Purity
Chemical Name
CAS Number
PubChem ID
InChI Key
SMILES
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 55.52 | 100 | |
| Ethanol | 13.88 | 25 |
Preparing Stock Solutions for AM 251
The following data is based on the product molecular weight 555.24.
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.80 mL | 9.01 mL | 18.01 mL |
| 5 mM | 0.36 mL | 1.80 mL | 3.60 mL |
| 10 mM | 0.18 mL | 0.90 mL | 1.80 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
Calculators
Background References
References are publications that support the biological activity of the product. See our Citations tab to view 945 publications citing the usage of this product.
- Seely AM-251 and rimon. act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies. Neuropharmacology 2012 PMID: 22771770
- Ellermann Endocannabinoids inhibit the induction of virulence in enteric pathogens. Cell 2020 PMID: 33031742
- Ryberg The orphan receptor GPR55 is a novel cannabinoid receptor. Br.J.Pharmacol. 2007 PMID: 17876302
- Gatley Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors. Life Sci. 1997 PMID: 9335234
- Pertwee Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci. 2005 PMID: 15670612
- Lan Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J.Med.Chem. 1999 PMID: 10052983
- Gatley 125I-labeled AM 251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors. Eur.J.Pharmacol. 1996 PMID: 8836622
Product Documents for AM 251
Certificate of Analysis
To download a Certificate of Analysis, please enter a lot or batch number in the search box below.
Product Specific Notices for AM 251
For research use only
Related Research Areas
Citations for AM 251
Customer Reviews for AM 251 (1)
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Species: MouseAssay Type: In VitroCell Line/Tissue: auditory brainstem(MNTB)Verified Customer | Posted 09/18/2018bath application of the CB1R antagonist AM251 (5 µM)
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