Glibenclamide

Glyburide, Glybenclamide, Micronase, Diabeta
An Activator of TRPA1 Channel and a Blocker of KATP Channels
    Cat #: G-150
    Alternative Name Glyburide, Glybenclamide, Micronase, Diabeta
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 494
    Purity: >99%
    Form Lyophilized powder.
    Effective concentration 1-100 µM.
      • Glibenclamide
    Chemical name 5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide.
    Molecular formula C23H28ClN3O5S.
    CAS No.: 10238-21-8.
    PubChem CID 3488
    Activity 1-100 µM Glibenclamide activates human TRPA1 expressing cells1.
      • Babes, A. et al. (2013) Eur. J. Pharmacol. 704, 15.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Up 200 mM in DMSO. Centrifuge all product preparations before use (5,000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
      • Glibenclamide
        Alomone Labs Glibenclamide activates TRPA1 channels expressed in HEK-293 cells. 
        Dose-response curve for the activation of human TRPA1 expressing HEK-293 cells loaded with Calcium 5 dye for changes in intracellular Ca2+ measurements. Calcium signal was apparent with 50 and 100 µM Glibenclamide (#G-150).
    References - Scientific background
    • 1. Babes, A. et al. (2013) Eur. J. Pharmacol. 704, 15.
    • 2. Caffes, N. et al. (2015) Int. J. Mol. Sci. 16, 4973.
    • 3. Kimber-Trojnar, Z. et al. (2008) Pharmacol. Rep. 60, 308.
    • 4. Khanna, A. et al. (2014) Neurosurg. Focus 36, 11.
    • 5. Simard, J.M. et al. (2014) Neurocrit. Care 20, 319.
      • Glibenclamide is a member of the sulfonylurea class of drugs, an anti-diabetic that inhibits KATP channels in pancreatic β-cells, leading to increased insulin release. Sulfonylurea drugs work by inhibiting sulfonylurea receptor 1 (SUR1). In addition, this drug acts as aTRPA1 agonist and demonstrates pleiotropic protective effects in acute CNS injury. Glibenclamide activates human TRPA1 in a concentration range that is commonly used to inhibit KATP channels in vitro. It has an EC50 value isof 48 nM at pH 7.45.

        Glibenclamide exhibits adverse effects such as abdominal pain, gastrointestinal disturbances and nocturia1,2. It is a weak acid, lipid soluble, with an oral clearance ranging from 11.2 to 230 l/h, with an elimination half-life estimated at about 4 h3.

        Promising preclinical results suggest that glibenclamide significantly reduces cerebral edema and lowers the rate of hemorrhagic conversion following ischemic stroke. In non-lethal models, glibenclamide reduces brain swelling and infarct volume and improves neurological function. In lethal models of malignant cerebral edema, glibenclamide reduces edema, brain swelling, and mortality3,4.

    Target TRPA1, KATP channels
    Last update: 02/09/2019

    Glibenclamide (#G-150) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use