NLRP3 inflammasome inhibitor - Glybenclamide
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NLRP3 inflammasome inhibitor - Proton pump inhibitor
NLRP3 inflammasome inhibitor
Glybenclamide, also known as glyburide, is an ATP-sensitive potassium channel inhibitor and an inhibitor of the NLRP3 inflammasome [1-3].
THE NLRP3 INFLAMMASOME:
The NLRP3 inflammasome is an innate immune sensor that is activated by a two-step process; a first signal (‘priming’) provided mainly by bacterial components or endogenous cytokines involves NF-κB induction, while the second signal provided by a wide array of stimuli including microbial toxins, endogenous molecules or crystalline substances and leads to inflammasome assembly and activation. This triggers inflammasome multimerization and caspase-1 activation with the subsequent cleavage of interleukin-1β (IL-1β)/IL-18 and the pore-forming protein Gasdermin D (GSDMD) into their active forms. Additionally, the activation of the inflammasome also leads to alarmin secretion and pyroptosis, a form of immunogenic cell death.
MODE OF ACTION OF GLYBENCLAMIDE:
Specifically, glybenclamide inhibits NLRP3 inflammasome activation by inducing the closure of ATP-sensitive K+ channels, and thereby raising the intracellular K+ concentration. This inhibitor works downstream of the ATP receptor P2X7, and upstream of NLRP3 . Of note, its inhibitory activity appears to be specific for the NLRP3 inflammasome as it does not impact NLRC4- or NLRP1-mediated responses [1, 2].
KEY FEATURES OF GLYBENCLAMIDE:
- Potent inhibitor of the NLRP3 inflammasome
- Potent inhibitor of the ATP-sensitive potassium channel
- Each lot is highly pure (≥98%) and functionally tested
Read our review on the NLRP3 inflammasome.
1. Zahid A. et al., 2019. Pharmacological Inhibitors of the NLRP3 Inflammasome. Front Immunol. 10:2538.
2. Lamkanfi M. et al., 2009. Glyburide inhibits the Cryopyrin/Nalp3 inflammasome. J. Cell Biol., 187: 61 - 70.
3. Dostert C. et al., 2009. Malarial hemozoin is a Nalp3 inflammasome activating danger signal. PLoS One. 4(8):e6510.
Working concentration: 20-200 μg/ml
CAS Number: 10238-21-8
Molecular weight: 494 g/mol
Solubility: Soluble in DMSO (25 mg/ml) and ethanol (5 mg/ml)
- Purity ≥ 98% (UHPLC).
- The inhibitory activity of the product has been validated in inflammasome cellular assays using THP1-Null2 and HEK-Blue™ IL-1β cells.
- The absence of bacterial contamination (e.g. lipoproteins and endotoxins) has been confirmed using HEK-Blue™ TLR2 and HEK‑Blue™ TLR4 cells.
- 1 g of Glybenclamide (glyburide) provided as a powder
Product is shipped at room temperature.
Upon receipt, store at room temperature (15-25 °C).
Resuspended product is stable for at least 6 months when properly stored.
Avoid repeated freeze-thaw cycles.Back to the top
Chemical structure of Glybenclamide:
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