An activator of SUR1 linked to Kir6.2 (EC50 = 14.1 µM in a FLIPR assay using HEK293 cells); activates SUR2A/Kir6.2 and SUR2B/Kir6.2 channels in HEK293T cells in a patch-clamp assay at 30 and 300 µM; inhibits glucose-induced insulin release from isolated rat pancreatic β cells and induces relaxation of isolated rat aortic rings precontracted with potassium chloride (IC50s = 22.6 and 22.4 µM

Diazoxide – 100 mg

Brand:
Cayman
CAS:
364-98-7
Storage:
-20
UN-No:
Non-Hazardous - /

Diazoxide is an activator of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = 14.1 µM in a FLIPR assay using HEK293 cells).{36318} It also activates SUR2A/Kir6.2 and SUR2B/Kir6.2 channels in HEK293T cells in a patch-clamp assay when used at concentrations of 30 and 300 µM.{48765} Diazoxide inhibits glucose-induced insulin release from isolated rat pancreatic β cells and induces relaxation of isolated rat aortic rings precontracted with potassium chloride (IC50s = 22.6 and 22.4 µM, respectively).{48766} It reduces mean arterial pressure and cerebral blood flow in spontaneously hypertensive rats when administered intravenously as a 5 mg/kg bolus dose.{48767} Diazoxide (50 mg/kg, i.p.) increases blood glucose levels in mice.{48768} Formulations containing diazoxide have been used in the treatment of hypoglycemia.  

 

Add to quotes
SKU: - Category:

Description

An activator of SUR1 linked to Kir6.2 (EC50 = 14.1 µM in a FLIPR assay using HEK293 cells); activates SUR2A/Kir6.2 and SUR2B/Kir6.2 channels in HEK293T cells in a patch-clamp assay at 30 and 300 µM; inhibits glucose-induced insulin release from isolated rat pancreatic β cells and induces relaxation of isolated rat aortic rings precontracted with potassium chloride (IC50s = 22.6 and 22.4 µM, respectively); reduces mean arterial pressure and cerebral blood flow in spontaneously hypertensive rats at an intravenous 5 mg/kg bolus dose; increases blood glucose levels in mice at 50 mg/kg i.p.

Formal name: 7-chloro-3-methyl-1,1-dioxide-2H-1,2,4-benzothiadiazine

Synonyms:  NSC 64198|NSC 76130|SRG 95213

Molecular weight: 230.7

CAS: 364-98-7

Purity: ≥99%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Endocrinology & Metabolism

Related products

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

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 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 - 50 mg

    Available on backorder

    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 50 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 - 50 mg

    Available on backorder

    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
    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