A sulfonylurea; an inhibitor of SUR1 linked to Kir6.2 (IC50 = 4.3 nM); binds to RINm5F microsomes (Kd = 0.3 nM); inhibits 86Rb+ efflux from intact RINm5 cells (K0.5 = 0.06 nM); reduces blood glucose levels and increases the activity of hepatic GST and G6PDH in an STZ-induced rat model of diabetes at 5 mg/kg; inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed BMDMs; reduces lesion growth in mice infected with L. mexicana at 80 mg/ml

Glyburide (potassium salt) – 10 g

Brand:
Cayman
CAS:
52169-36-5
Storage:
-20
UN-No:
Non-Hazardous - /

Glyburide is a sulfonylurea and an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (IC50 = 4.3 nM).{22674} It binds to microsomes derived from RINm5F pancreatic β-cells (Kd = 0.3 nM) and inhibits 86Rb+ efflux from intact RINm5 cells with a half-maximal inhibition (K0.5) value of 0.06 nM.{22672} Glyburide (5 mg/kg) reduces blood glucose levels and increases the activity of hepatic glutathione-S-transferase (GST) and glucose-6-phosphate dehydrogenase (G6PDH) in a rat model of diabetes induced by streptozotocin (STZ; Item No. 13104).{43282} It inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed bone marrow-derived macrophages (BMDMs).{22671} Glyburide (80 mg/ml) also reduces lesion growth in mice infected with L. mexicana.{22673} Formulations containing glyburide have been used in the treatment of type 2 diabetes.  

 

Add to quotes
SKU: - Category:

Description

A sulfonylurea; an inhibitor of SUR1 linked to Kir6.2 (IC50 = 4.3 nM); binds to RINm5F microsomes (Kd = 0.3 nM); inhibits 86Rb+ efflux from intact RINm5 cells (K0.5 = 0.06 nM); reduces blood glucose levels and increases the activity of hepatic GST and G6PDH in an STZ-induced rat model of diabetes at 5 mg/kg; inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed BMDMs; reduces lesion growth in mice infected with L. mexicana at 80 mg/ml

Formal name: 5-chloro-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxy-benzamide, monopotassium salt

Synonyms:  Glibenclamide

Molecular weight: 532.1

CAS: 52169-36-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antiparasitics|Antiprotozoals||Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Infectious Disease|Parasitic Diseases|Leishmaniasis

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 – 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
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 10 µg

    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 – 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
    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