A β1-adrenergic receptor partial agonist (EC50 = 80 nM for the generation of cAMP in neonatal rat cardiomyocyte cultures); increases spontaneous contraction of isolated rat right atria (EC50 = 4.67 nM); increases heart rate in beagle dogs (ED50 = 3.2 µg/kg) and a rat model of spontaneous heart failure (ED50 = 6 µg/kg)

Xamoterol (hemifumarate) – 25 mg

Brand:
Cayman
CAS:
73210-73-8
Storage:
-20
UN-No:
Non-Hazardous - /

Xamoterol is a partial agonist of β1-adrenergic receptors (β1-ARs) with an EC50 value of 80 nM for the generation of cyclic AMP (cAMP) in neonatal rat cardiomyocyte cultures.{41648} It increases spontaneous contraction of isolated rat right atria (EC50 = 4.67 nM).{41649} In vivo, xamoterol increases heart rate in beagle dogs (ED50 = 3.2 µg/kg) and in a rat model of spontaneous heart failure (ED50 = 6 µg/kg), an effect that is reversed by the selective β1-AR antagonist betaxolol (Item No. 18625) but not the selective β2-AR antagonist ICI 118551 (Item No. 15591).{41648,41647} Formulations containing xamoterol have been used in the treatment of heart failure.  

 

Available on backorder

Add to quotes
SKU: 24267 - 25 mg Category:

Description

A β1-adrenergic receptor partial agonist (EC50 = 80 nM for the generation of cAMP in neonatal rat cardiomyocyte cultures); increases spontaneous contraction of isolated rat right atria (EC50 = 4.67 nM); increases heart rate in beagle dogs (ED50 = 3.2 µg/kg) and a rat model of spontaneous heart failure (ED50 = 6 µg/kg)

Formal name: N-[2-[[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-4-morpholinecarboxamide, (E)-2-butenedioate (2:1)

Synonyms:  ICI 118587

Molecular weight: 397.4

CAS: 73210-73-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Heart|Arrhythmia

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 – 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
  • 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
  • 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 – 25 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 - 25 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