A non-selective β-adrenergic receptor antagonist (Kds = 1.78

Carvedilol – 100 mg

Brand:
Cayman
CAS:
72956-09-3
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Carvedilol is a non-selective antagonist of the β-adrenergic receptor (β-AR; Kds = 1.78, 0.4, and 5.01 nM for β1-, β2-, and β3-ARs, respectively).{25151} It also binds to α1-, but not α2-, adrenergic receptors (Kis = 0.81 and 3,400 nM, respectively).{25150} Carvedilol reverses increases in heart rate induced by the β1-AR agonist isoproterenol (Item No. 15592) in isolated guinea pig atria (Kb = 0.8 nM) and induces relaxation of isolated precontracted guinea pig trachea (Kb = 1.3 nM).{43226} It prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia with an ED50 value of 0.25 mg/kg.{25150} Carvedilol also inhibits the contractile response to the α1-AR agonist norepinephrine in isolated rabbit aorta (Kb = 11 nM).{43226} It decreases systolic blood pressure and heart rate in rat models of hypertension, including spontaneously hypertensive, renal hypertensive, and deoxycorticosterone acetate-treated rats when administered at doses ranging from 3 to 30 mg/kg.{43227} Carvedilol also activates cardioprotective signaling through β-arrestin and ERK1/2 activation.{25152,25153,23372} Formulations containing carvedilol have been used in the treatment of congestive heart failure and hypertension.  

 

Add to quotes
SKU: - Category:

Description

A non-selective β-adrenergic receptor antagonist (Kds = 1.78, 0.4, and 5.01 nM for β1-, β2-, and β3-ARs, respectively); also binds to α1-, but not α2-, adrenergic receptors (Kis = 0.81 and 3,400 nM, respectively); reverses increases in heart rate induced by isoproterenol in isolated guinea pig atria (Kb = 0.8 nM); induces relaxation of isolated precontracted guinea pig trachea (Kb = 1.3 nM); prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia (IC50 = 0.25 mg/kg); inhibits the contractile response to norepinephrine in isolated rabbit aorta (Kb = 11 nM); decreases systolic blood pressure and heart rate in rat models of hypertension at 3-30 mg/kg

Formal name: 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol

Synonyms:  BM 14190

Molecular weight: 406.5

CAS: 72956-09-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cardiovascular System|Vasculature|Vasodilation

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) – 250 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 - 250 mg

    Available on backorder

    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 – 10 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 - 10 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 – 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
    View product page