Home Metabolism PPAR agonist - GABA Receptor agonist Glabridin For research use only.

Glabridin

Synonyms: Q-100692, KB-289522, LS-176045

Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.

Glabridin Chemical Structure

Glabridin Chemical Structure

CAS No. 59870-68-7

Purity & Quality Control

Batch: S378601 DMSO]64 mg/mL]false]]]false]]]false Purity: 99.87%
99.87

Glabridin Related Products

Signaling Pathway

PPAR Signaling Pathways

PPAR Signaling Pathway

Biological Activity

Description Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
Targets
PPARγ [1]
(Cell-free assay)		 α1β2γ2 (GABAA receptor) [3] α1β3γ2 (GABAA receptor) [3] α1β2 (GABAA receptor) [3] α1β1γ2 (GABAA receptor) [3]
6.3 μM(EC50) 6.83 μM(EC50) 9.63 μM(EC50) 17.23 μM(EC50)
In vitro
In vitro Glabridin induces dose-dependent increase in estrogenic activity and cell proliferation in Ishikawa cells. Glabridin exerts estrogenic activity via the ER-α-SRC-1-co-activator complex[1]. Glabridin has substantial neuroprotective effects, as indicated by the reduced cell death, apoptosis, DNA fragmentation, probably through the regulation of bcl-2, Bax and caspase-3 which are all closely related to cell apoptotic process[2].
Cell Research Cell lines Ishikawa cells
Concentrations 1nM to 10μM
Incubation Time 72 h
Method The effect of the extracts on cell proliferation are estimated using MTT assay. Briefly, 10μL of 5 mg/ml MTT is added to each well after incubation with test compounds for 72 h. DMSO is then added to dissolve the formazan and the plate read at 595 nm. The cell proliferation of control cells is 100.00% and any increase or decrease in cell proliferation of treated cells is compared to the control cells. All experimental conditions are assayed in triplicate.
In Vivo
In vivo Glabridin at 25mg/kg by intraperitoneal injection, but not at 5mg/kg, significantly decreases the focal infarct volume, cerebral histological damage and apoptosis in MCAO rats compared to sham-operated rats. Glabridin significantly attenuates the level of brain malonyldialdehyde (MDA) in MCAO rats, while it elevates the level of two endogenous antioxidants in the brain, i.e. superoxide dismutase (SOD) and reduced glutathione (GSH). Co-treatment with glabridin significantly inhibits the staurosporine-induced cytotoxicity and apoptosis of cultured rat cortical neurons in a concentration-dependent manner. Consistently, glabridin significantly reduces the DNA laddering caused by staurosporine in a concentration-dependent manner. Glabridin has a neuroprotective effect via modulation of multiple pathways associated with apoptosis. Glabridin appears to achieve steady state concentrations slowly in humans. The limited penetration of glabridin into the brain due to the activity of P-glycoprotein in the blood-brain barrier may also lessen the activity of glabridin at low doses[2].
Animal Research Animal Models Male healthy Sprague-Dawley rats
Dosages 5 mg/kg and 25 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 324.37 Formula

C20H20O4
CAS No. 59870-68-7 SDF Download Glabridin SDF
Smiles CC1(C=CC2=C(O1)C=CC3=C2OCC(C3)C4=C(C=C(C=C4)O)O)C
Storage (From the date of receipt)

In vitro
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DMSO : 64 mg/mL ( (197.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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