Product overview
| Name | AM251 |
| Description | Potent, selective CB1 receptor antagonist / inverse agonist |
| Purity | >98% |
| Customer comments | It (AM251) works - bang for your buck! Works as described! Great technical support. Verified customer, UC Denver Another quality product from Hello Bio - AM251 works as expected in our experiments and at a good price as well. We always order with confidence from Hello Bio, and are often surprised at how quickly we receive our products. Verified customer, University of South Carolina |
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Biological Data
| Biological description | AM251 is a potent and selective prototypic cannabinoid 1 receptor (CB1) antagonist / inverse agonist (IC50 = 8 nM and Ki = 7.49 nM).
AM251 attenuates responses to established cannabinoid receptor agonists in vitro or in vivo.
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Solubility & Handling
| Storage instructions | Room temperature |
| Solubility overview | Soluble in DMSO (100 mM) and in ethanol (25 mM) |
| Handling | This compound is light sensitive; we therefore recommend protecting the solid material and solutions from exposure to light.
We therefore recommend:
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| Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
| Chemical name | N-(Piperidin-1-yl)-5-(4-iodophenyl) -1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-car boxamide |
| Molecular Weight | 555.24 |
| Chemical structure | ![AM 251 [183232-66-8] Chemical Structure](https://hellobio.com/media/catalog/product//h/b/hb2776.png "AM 251 [183232-66-8]") |
| Molecular Formula | C22H21Cl2IN4O |
| CAS Number | 183232-66-8 |
| PubChem identifier | 2125 |
| SMILES | CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I |
| Source | Synthetic |
| InChi | InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30) |
| InChiKey | BUZAJRPLUGXRAB-UHFFFAOYSA-N |
| MDL number | MFCD01861181 |
| Appearance | White solid |
References for AM251
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AM-251 and SR141716 act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies.
Seely et al (2012) Neuropharmacology 63(5) : 905-15 -
The cannabinoid CB1 receptor antagonists SR141716 and AM251 directly potentiate GABA(A) receptors.
Baur et al (2012) Br J Pharmacol 165(8) : 2479-84 -
Cannabinoid CB1 receptor antagonists attenuate cocaine's rewarding effects: experiments with self-administration and brain-stimulation reward in rats.
Xi et al (2008) Neuropsychopharmacology 33(7) : 1735-45 -
The orphan receptor GPR55 is a novel cannabinoid receptor.
Ryberg et al (2007) Br J Pharmacol 152(7) : 1092-101. -
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.
Lan et al (1999) J Med Chem 42(4) : 769-76
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