A positive allosteric modulator of adenosine A3 receptors; reduces dissociation of I-AB-MECA from A3 receptors and increases the efficacy

LUF6000 – 500 µg

Brand:
Cayman
CAS:
890087-21-5
Storage:
-20
UN-No:
Non-Hazardous - /

LUF6000 is a positive allosteric modulator of adenosine A3 receptors.{42969} It reduces dissociation of the agonist I-AB-MECA from A3 receptors and increases the efficacy, but not potency, of 2-Cl-IB-MECA-induced inhibition of forskolin-stimulated cAMP accumulation by 45% in CHO cells expressing the human receptor when used at a concentration of 10 μM. LUF6000 (100 μg/kg, three times per day) reduces joint edema and decreases levels of PI3K, IKK, IκB, and NF-κB in peripheral blood mononuclear cells (PBMCs) in a rat model of adjuvant-induced arthritis.{42970} It reduces knee edema in a rat model of osteoarthritis induced by monosodium iodoacetate (MIA) when administered at a dose of 100 μg/kg twice per day.  

 

Available on backorder

Add to quotes
SKU: 28437 - 500 µg Category:

Description

A positive allosteric modulator of adenosine A3 receptors; reduces dissociation of I-AB-MECA from A3 receptors and increases the efficacy, but not potency, of 2-Cl-IB-MECA-induced inhibition of forskolin-stimulated cAMP accumulation by 45% in CHO cells expressing the human receptor at 10 μM; reduces joint edema and decreases levels of PI3K, IKK, IκB, and NF-κB in PBMCs in a rat model of adjuvant-induced arthritis at 100 μg/kg, three times per day; reduces knee edema in a rat model of MIA-induced osteoarthritis at 100 μg/kg twice per day

Formal name: 2-cyclohexyl-N-(3,4-dichlorophenyl)-3H-imidazo[4,5-c]quinolin-4-amine

Synonyms: 

Molecular weight: 411.3

CAS: 890087-21-5

Purity: ≥98%

Formulation: A solid

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 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 - 25 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 1 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 1 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
  • 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