In my cart

You have no items in your shopping cart.

Data

Product overview

  • Name
    AM251
  • Short description
    Potent, selective CB1 receptor antagonist / inverse agonist
  • 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 shows ~306-fold selectivity over CB2 receptors. Structural analog of SR141716A.


    Also acts as a potent GPR55 orphan receptor agonist (EC50 = 39 nM) and shows activity at the µ-opioid receptor (MOR) (Ki = 251 nM). Additionally, directly potentiates GABAreceptors.


    AM251 attenuates responses to established cannabinoid receptor agonists in vitro or in vivo.


    Blocks heterosynaptic long term depression (LTD).

  • Biological action
    Antagonist
  • 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

  • Citations

Images

Properties

  • 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]
  • 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

Storing and Using Your Product

  • 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.


    Ongoing solubility of AM251 in aqueous solutions can be unpredictable and the compound can precipitate out of solution.

    We therefore recommend:

    1. If possible, make up solutions and use immediately. Do not store solutions.
    2. When creating your stock solutions, ensure the compound is fully dissolved in DMSO (use heat to achieve this if necessary).
    3. Mix the compound with ACSF immediately before use. You can also heat your ACSF solution to ~42°C before addition of AM251.
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for AM251

  • 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
    PubMedID: 22771770
  • 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
    PubMedID: 17728698
  • Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.

    Lan et al (1999) J Med Chem 42(4) : 769-76
    PubMedID: 10052983
  • The orphan receptor GPR55 is a novel cannabinoid receptor.

    Ryberg et al (2007) Br J Pharmacol 152(7) : 1092-101.
    PubMedID: 17876302
  • The cannabinoid CB1 receptor antagonists SR141716 and AM251 directly potentiate GABA(A) receptors.

    Baur et al (2012) Br J Pharmacol 165(8) : 2479-84
    PubMedID: 21470203
Support & Resources

Reviews & Product Guides

Reviews

  • Verified customer, University of South Carolina

    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, UC Denver

    It (AM 251) works - bang for your buck! Works as described! Great technical support.