An adenosine A3 receptor agonist (Ki = 1.7 nM); selective for adenosine A3 over A1 and A2 receptors (Kis = 55.3 and 3

Piclidenoson – 1 mg

Brand:
Cayman
CAS:
152918-18-8
Storage:
-20
UN-No:
Non-Hazardous - /

Piclidenoson is an adenosine A3 receptor agonist (Ki = 1.7 nM).{52557} It is selective for adenosine A3 over A1 and A2 receptors (Kis = 55.3 and 3,099 nM, respectively). In vivo, piclidenoson (100 µg/kg) reduces wall thickening in a rabbit model of ischemia-reperfusion injury induced by coronary artery occlusion, an effect that can be reversed by the adenosine receptor antagonist 8-p-sulfophenyl theophylline.{52556} It reduces hepatocellular tumor growth, liver inflammation, and neuropathy in a rat model of bone-residing breast cancer and decreases the number of lung metastases in a model of metastatic murine melanoma.{52557} Piclidenoson (1 and 3 mg/kg) also reduces colonic inflammatory cell infiltration and damage in a mouse model of colitis induced by dextran sulfate (DSS; Item No. 23250) and in IL-10-/- mice.{52558}  

 

Available on backorder

Add to quotes
SKU: 28445 - 1 mg Category:

Description

An adenosine A3 receptor agonist (Ki = 1.7 nM); selective for adenosine A3 over A1 and A2 receptors (Kis = 55.3 and 3,099 nM, respectively); reduces wall thickening in a rabbit model of ischemia-reperfusion injury induced by coronary artery occlusion at 100 µg/kg; reduces hepatocellular tumor growth, liver inflammation, and neuropathy in a rat model of bone-residing breast cancer and the number of lung metastases in a model of metastatic murine melanoma; reduces colonic inflammatory cell infiltration and damage in a mouse model of DSS-induced colitis and in in IL-10-/- mice at 1 and 3 mg/kg

Formal name: 1-deoxy-1-[6-[[(3-iodophenyl)methyl]amino]-9H-purin-9-yl]-N-methyl-β-D-ribofuranuronamide

Synonyms:  CF-101|IB-MECA

Molecular weight: 510.3

CAS: 152918-18-8

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • 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 – 10 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 - 10 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 – 500 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 - 500 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 50 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 - 50 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 5 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page