A calcium channel inhibitor; inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-adrenergic

Fantofarone – 5 mg

Brand:
Cayman
CAS:
114432-13-2
Storage:
-20
UN-No:
Non-Hazardous - /

Fantofarone is a calcium channel inhibitor.{47567} It selectively inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-adrenergic, muscarinic, and histamine H2 receptors in rat heart homogenates (IC50s = >10, 4, >10, and >10 µM, respectively), and the serotonin receptor subtypes 5-HT1 and 5-HT2, as well as histamine H1 and adenosine A1 receptors, in rat brain homogenates (IC50s = >10, >10, 4, and >10 µM, respectively). Fantofarone inhibits peak calcium current in depolarized and hyperpolarized L-type voltage-gated calcium channels (IC50s = 1.4 and 150 nM, respectively).{47568} It inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC50s = 5.64 and 96 nM, respectively).{47567} It enhances recovery of cardiac output during reperfusion of isolated rat hearts when used at a concentration of 10 nM.{47569} Fantofarone prevents angioplasty-induced vasospasms in the femoral artery in a rabbit model of focal atherosclerosis when administered at a dose of 50 µg/kg.{47570}  

 

Available on backorder

Add to quotes
SKU: 26381 - 5 mg Category:

Description

A calcium channel inhibitor; inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-adrenergic, muscarinic, and histamine H2 receptors in rat heart homogenates (IC50s = >10, >10, 4, and >10 µM, respectively), and the serotonin receptor subtypes 5-HT1 and 5-HT2, as well as histamine H1 and adenosine A1 receptors, in rat brain homogenates (IC50s = >10, 4, >10, and >10 µM, respectively); inhibits peak calcium current in depolarized and hyperpolarized L-type voltage-gated calcium channels (IC50s = 1.4 and 150 nM, respectively); inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC50s = 5.64 and 96 nM, respectively); enhances recovery of cardiac output during reperfusion of isolated rat hearts at 10 nM; prevents angioplasty-induced vasospasms in the femoral artery in a rabbit model of focal atherosclerosis at 50 µg/kg

Formal name: 3,4-dimethoxy-N-methyl-N-[3-[4-[[2-(1-methylethyl)-1-indolizinyl]sulfonyl]phenoxy]propyl]-benzeneethanamine

Synonyms:  SR 33557

Molecular weight: 550.7

CAS: 114432-13-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Heart||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Cell Biology|Cell Signaling|Calcium Mobilization

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 – 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 potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 5 mg

    Available on backorder

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

    1,2-Dipalmitoyl-sn-glycero-3-PC – 100 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 - 100 mg

    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) – 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