A CysLT1 receptor antagonist (IC50 = 0.014 μM in a cell-based calcium mobilization assay); selective for CysLT1 over CysLT2 receptors (IC50 = 58 μM); inhibits LTD4-induced mucus secretion in isolated guinea pig trachea (IC50 = 0.6 μM); inhibits ovalbumin-induced increases in tracheal mucus secretion in ovalbumin-sensitized guinea pigs by 65% at 5 μM; inhibits LTD4-induced bronchoconstriction in anesthetized guinea pigs (ED50 = 61 nmol/kg

Zafirlukast – 10 mg

Brand:
Cayman
CAS:
107753-78-6
Storage:
-20
UN-No:
Non-Hazardous - /

Zafirlukast is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50 = 0.014 μM in a cell-based calcium mobilization assay).{49502} It is selective for CysLT1 over CysLT2 receptors (IC50 = 58 μM). It inhibits mucus secretion induced by leukotriene D4 (LTD4; Item No. 20310) in isolated guinea pig trachea (IC50 = 0.6 μM).{46532} Zafirlukast (5 μM) inhibits ovalbumin-induced increases in tracheal mucus secretion in ovalbumin-sensitized guinea pigs by 65%. It inhibits LTD4-induced bronchoconstriction in anesthetized guinea pigs (ED50 = 61 nmol/kg, i.v.).{10911} Formulations containing zafirlukast have been used in the prophylaxis and chronic treatment of asthma.  

 

Available on backorder

Add to quotes
SKU: 10008282 - 10 mg Category:

Description

A CysLT1 receptor antagonist (IC50 = 0.014 μM in a cell-based calcium mobilization assay); selective for CysLT1 over CysLT2 receptors (IC50 = 58 μM); inhibits LTD4-induced mucus secretion in isolated guinea pig trachea (IC50 = 0.6 μM); inhibits ovalbumin-induced increases in tracheal mucus secretion in ovalbumin-sensitized guinea pigs by 65% at 5 μM; inhibits LTD4-induced bronchoconstriction in anesthetized guinea pigs (ED50 = 61 nmol/kg, i.v.)

Formal name: [3-[[2-methoxy-4-[[[(2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]-carbamic acid, cyclopentyl ester

Synonyms: 

Molecular weight: 575.7

CAS: 107753-78-6

Purity: ≥97%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Pulmonary Diseases|Asthma||Research Area|Lipid Biochemistry|Lipoxygenase Pathways

Related products

  • 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) – 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 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
  • 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