An adenosine A3 receptor antagonist (Ki = 4.03 nM for the recombinant human receptor); >2

VUF 5574 – 5 mg

Brand:
Cayman
CAS:
280570-45-8
Storage:
-20
UN-No:
Non-Hazardous - /

VUF 5574 is an antagonist of the adenosine A3 receptor (Ki = 4.03 nM for the recombinant human receptor).{49476} It is greater than 2,500-fold selective for adenosine A3 over A1 and A2A receptors. VUF 5574 (100 nM) decreases phosphorylation of ERK1/2 induced by adenosine (Item No. 21232) in isolated porcine coronary artery smooth muscle cells.{49477} It increases oxygen-glucose deprivation-induced reductions in the amplitude of field excitatory postsynaptic potentials (EPSPs) in a rat hippocampal slice model of ischemia when used at a concentration of 100 nM.{49478} VUF 5574 (2 µg, intracisternal) reduces sodium nitroprusside-induced heart rate increases in rats.{49479}  

 

Available on backorder

Add to quotes
SKU: 27676 - 5 mg Category:

Description

An adenosine A3 receptor antagonist (Ki = 4.03 nM for the recombinant human receptor); >2,500-fold selective for adenosine A3 over A1 and A2A receptors; decreases adenosine-induced phosphorylation of ERK1/2 in isolated porcine coronary artery smooth muscle cells at 100 nM; increases oxygen-glucose deprivation-induced reductions in the amplitude of field EPSPs in a rat hippocampal slice model of ischemia at 100 nM; reduces sodium nitroprusside-induced heart rate increases in rats at 2 µg intracisternally

Formal name: N-(2-methoxyphenyl)-N’-[2-(3-pyridinyl)-4-quinazolinyl]-urea

Synonyms: 

Molecular weight: 371.4

CAS: 280570-45-8

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Stroke||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells||Research Area|Neuroscience|Neuroprotection|Ischemia

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 powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 50 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 - 50 mg

    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 – 10 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 - 10 mg

    Available on backorder

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

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 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 - 10 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page