A phenylalkylamine L-type calcium channel blocker; blocks recombinant rat L-type calcium channels expressed in tsA201 cells (IC50s = 782 and 8

(±)-Methoxyverapamil (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
16662-46-7
Storage:
-20
UN-No:
Non-Hazardous - /

(±)-Methoxyverapamil is a phenylalkylamine L-type calcium channel blocker and methoxy derivative of verapamil (Item No. 14288).{38991} (±)-Methoxyverapamil blocks recombinant rat L-type calcium channels expressed in tsA201 cells with IC50 values of 782 and 8,000 nM at holding potentials of 10 and -60 mV, respectively. It blocks maitotoxin-induced calcium influx in NIH3T3 fibroblasts (IC50 = 16 μM) and inhibits histamine-induced acid secretion by primary enriched guinea pig parietal cells (IC50 = 10.9 μM).{38992,38993} (±)-Methoxyverapamil binds to rat myocardial membranes (IC50 = 16 nM) and inhibits electrically-stimulated contractions in rat right myocardial ventricular strips (EC50 = 1.95 μM).{38994} In conscious, ovariectomized, post-partum rats, it decreases blood pressure by 30 mm Hg and induces 60% inhibition of uterine contractions when administered at doses of 204 and 324 μg/kg, respectively.{38995}  

 

Available on backorder

Add to quotes
SKU: 24270 - 10 mg Category:

Description

A phenylalkylamine L-type calcium channel blocker; blocks recombinant rat L-type calcium channels expressed in tsA201 cells (IC50s = 782 and 8,000 nM at holding potentials of 10 and -60 mV, respectively); blocks maitotoxin-induced calcium influx in NIH3T3 fibroblast cells (IC50 = 16 μM); inhibits histamine-induced acid secretion by primary enriched guinea pig parietal cells (IC50 = 10.9 μM); binds to rat myocardial membranes (IC50 = 16 nM); inhibits electrically-stimulated contractions in rat right myocardial ventricular strips (EC50 = 1.95 μM); decreases blood pressure and inhibits uterine contractions in conscious, ovariectomized, post-partum rats (204 and 324 μg/kg, respectively)

Formal name: α-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-3,4,5-trimethoxy-α-(1-methylethyl)-benzeneacetonitrile, monohydrochloride

Synonyms:  Gallopamil|NSC 274966

Molecular weight: 521.1

CAS: 16662-46-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Endocrinology & Metabolism|Reproductive Biology

Related products

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

    (R)-Roscovitine – 10 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 - 10 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) – 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
    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 – 1 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 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page