A piperazine derivative with cardioprotective activity; reduces INa in mouse myocytes expressing the long QT syndrome 3 mutant sodium channel DKPQ

Ranolazine (hydrochloride) – 100 mg

Brand:
Cayman
CAS:
95635-56-6
Storage:
-20
UN-No:
Non-Hazardous - /

Ranolazine is a piperazine derivative with cardioprotective activity.{25575,25576,25577,42415} It reduces the late sodium current (INa) in mouse myocytes expressing the long QT syndrome 3 mutant sodium channel DKPQ, ventricular myocytes isolated from a canine model of heart failure, guinea pig ventricular myocytes exposed to hydrogen peroxide or anemone toxin-II, and HEK293 cells expressing human Nav1.5 channels (IC50s = 5.9-15 μM) as well as the late potassium current (IKr) in canine ventricular myocytes and HEK293 cells (IC50s = 11.5 and 14.4 μM, respectively).{25575,25576} Ranolazine also inhibits radioligand binding to α1-, β1-, and β2-adrenergic receptors (Kis = 8.2-19.5, 1.4-8.6, and 0.5-14.8 μM, respectively).{25576} In vivo, ranolazine (480 μg/kg per min) reduces clofilium-induced prolongation of the QTc interval and Torsade de Pointes (TdP) in rabbits.{25577} Ranolazine also reduces interstitial collagen deposition as well as atrial natriuretic peptide (ANP; Item Nos. 24539 | 24276), connective tissue growth factor (CTGF), brain natriuretic peptide (BNP; Item No. 24541), and matrix metalloproteinase-2 (MMP-2) mRNA levels, and prevents left ventricular dilation in a mouse model of cardiotoxicity induced by doxorubicin (Item No. 15007).{42415}  

 

Add to quotes
SKU: - Category:

Description

A piperazine derivative with cardioprotective activity; reduces INa in mouse myocytes expressing the long QT syndrome 3 mutant sodium channel DKPQ, ventricular myocytes isolated from a canine model of heart failure, guinea pig ventricular myocytes exposed to hydrogen peroxide or anemone toxin-II, and HEK293 cells expressing human Nav1.5 channels (IC50s = 5.9-15 μM); reduces IKr in canine ventricular myocytes and HEK293 cells (IC50s = 11.5 and 14.4 μM, respectively); reduces clofilium-induced prolongation of the QTc interval and TdP in rabbits at 480 μg/kg per min; reduces interstitial collagen deposition as well as ANP, CTGF, BNP, and MMP-2 mRNA levels, and prevents left ventricular dilation in a mouse model of doxorubicin-induced cardiotoxicity,

Formal name: N-(2,6-dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazineacetamide, dihydrochloride

Synonyms:  RS 43285

Molecular weight: 500.5

CAS: 95635-56-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology||Research Area|Cardiovascular System|Heart|Arrhythmia

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 250 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 250 mg

    Available on backorder

    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
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 25 mg

    Available on backorder

    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
    View product page