An inhibitor of PDE3 (IC50 = 0.35 μM for human cardiac enzyme); selective for PDE3 over PDE1 and PDE2 (IC50s = 150 and 100 μM

Olprinone (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
119615-63-3
Storage:
-20
UN-No:
Non-Hazardous - /

Olprinone is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 0.35 μM for human cardiac enzyme).{51184} It is selective for PDE3 over PDE1 and PDE2 (IC50s = 150 and 100 μM, respectively). Olprinone induces relaxation of precontracted isolated rabbit renal and carotid arterial rings (IC50s = 40 and 103 nM, respectively).{51185} It reduces infarct size and improves cardiac function in a rat model of myocardial ischemia-reperfusion injury when administered at a dose of 0.6 mg/kg twice per day.{51186} Olprinone (0.2 mg/kg) reduces cortical and striatal damage, as well as reduces injured cerebral tissue nitrotyrosine formation, apoptosis, and levels of inducible nitric oxide synthase (iNOS), IL-1β, and intercellular adhesion molecule 1 (ICAM-1) in a rat model of cerebral ischemia-reperfusion injury.{51187} It inhibits neutrophil infiltration into the lungs and inhibits increases in serum levels of TNF-α and IL-6 in a rat model of LPS-induced lung inflammation when administered at a dose of 0.2 mg/kg.{51188}  

 

Available on backorder

Add to quotes
SKU: 28396 - 10 mg Category:

Description

An inhibitor of PDE3 (IC50 = 0.35 μM for human cardiac enzyme); selective for PDE3 over PDE1 and PDE2 (IC50s = 150 and 100 μM, respectively); induces relaxation of precontracted isolated rabbit renal and carotid arterial rings (IC50s = 40 and 103 nM, respectively); reduces infarct size and improves cardiac function in a rat model of myocardial ischemia-reperfusion injury at 0.6 mg/kg twice per day; reduces cortical and striatal damage, as well as reduces injured cerebral tissue nitrotyrosine formation, apoptosis, and levels of iNOS, IL-1β, and ICAM-1 in a rat model of cerebral ischemia-reperfusion injury at 0.2 mg/kg; inhibits neutrophil infiltration into lung and inhibits increases in serum levels of TNF-α and IL-6 in a rat model of LPS-induced lung inflammation at 0.2 mg/kg

Formal name: 1,2-dihydro-5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-3-pyridinecarbonitrile, monohydrochloride

Synonyms:  Loprinone

Molecular weight: 286.7

CAS: 119615-63-3

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • 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
  • 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
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 500 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 - 500 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