An AEA transport inhibitor with essentially no activity on the CB1 receptor

VDM11 – 25 mg

Brand:
Cayman
CAS:
313998-81-1
Storage:
-20
UN-No:
De Minimis - 1170 / 3

Numerous analogs of arachidonoyl ethanolamide (AEA) potentiate its biological activity. This potentiation is ascribed either to inhibition of AEA reuptake into neurons, or inhibition of fatty amide acyl hydrolase (FAAH) within the neurons.{10254,10647} VDM11 is an AEA transport inhibitor with essentially no activity on either the central cannabinoid receptor (CB1), peripheral cannabinoid receptor (CB2), or the vanilloid receptor 1 (VR1).{9577} However, VDM11 inhibits FAAH and monoacylglycerol lipase (MAGL) and may act as an alternative FAAH substrate.{14077} At a concentration of 3 µM, VDM11, like AM404, inhibits glutamergic synaptic transmission between hippocampal neurons.{12853} The mechanism of this effect may be a direct action on sodium channels. Thus, the use of anandamide analogs as uptake inhibitors and interpretation of the results must be undertaken with care.  

 

Available on backorder

Add to quotes
SKU: 10006731 - 25 mg Category:

Description

An AEA transport inhibitor with essentially no activity on the CB1 receptor, CB2 receptor, or TRPV1; inhibits FAAH and MAGL and may act as an alternative FAAH substrate; inhibits glutamergic synaptic transmission between hippocampal neurons at a concentration of 3 µM

Formal name: N-(4-hydroxy-2-methylphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide

Synonyms: 

Molecular weight: 409.6

CAS: 313998-81-1

Purity: >98%

Formulation: A solution in ethanol

Product Type|Biochemicals|Small Molecule Inhibitors|Fatty Acid Metabolism||Product Type|Biochemicals|Small Molecule Inhibitors|Glycerolipid Lipases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Lipid Biochemistry|Endocannabinoid/Endocannabinoid-like||Research Area|Lipid Biochemistry|Glycerolipids|Lipases||Research Area|Lipid Biochemistry|Lipid Transport||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 25 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 250 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 250 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 50 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page