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  3. Umbelopsisin A

Umbelopsisin A is a GABAA and GABAB non-selective agonist. Umbelopsisin A activates the GABAergic pathway, including notch signaling and fatty acid metabolism. Umbelopsisin A shows dual neuroprotection against glutamate excitotoxicity in vitro (reducing ROS and cell death) and in vivo. Umbelopsisin A can be used for the study of glaucoma and broader neurodegenerative disease applications.

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Umbelopsisin A

Umbelopsisin A Chemical Structure

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Description

Umbelopsisin A is a GABAA and GABAB non-selective agonist. Umbelopsisin A activates the GABAergic pathway, including notch signaling and fatty acid metabolism. Umbelopsisin A shows dual neuroprotection against glutamate excitotoxicity in vitro (reducing ROS and cell death) and in vivo. Umbelopsisin A can be used for the study of glaucoma and broader neurodegenerative disease applications[1].

In Vitro

Umbelopsisin A (0.5 μM-16 μM; 24 h; R28 cells) rescues R28 cells from Glu-induced excitotoxicity and reduces ROS production[1].
Umbelopsisin A (2 μM; 24 h; R28 cells) modulates gene expression in R28 cells, promoting axonogenesis and GABA-related pathways[1].
Umbelopsisin A (20 μM-400 μM; 24 h; R28 cells) acts as a GABA receptor agonist, directly binding to GABA_A and GABA_B receptors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: R28 cells
Concentration: 0.5 μM, 1 μM, 2 μM, 3 μM, 4 μM, 8 μM, 16 μM
Incubation Time: 24 h
Result: Partially restored glutamate (Glu)-induced cell viability reduction.
Significantly reduced Glu-induced R28 cell death and ROS production, with 2 μM showing significant protection.
At 16 μM, significantly reduced cell viability compared to the Glu group.
In Vivo

Umbelopsisin A (20 μM; Intravitreal; 1 μL) preserves retinal ganglion cells (RGCs) and improves visual function in NMDA-induced retinal injury in C57BL/6[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 8 weeks) bearing NMDA-induced retinal injury[1]
Dosage: 20 μM
Administration: Intravitreal; 1 μL
Result: RGCs density was significantly preserved in the central and mid-peripheral retina. NMDA-induced GCC thinning was significantly attenuated. f-ERG and f-VEP wave amplitudes were significantly improved.
Molecular Weight

365.38

Formula

C21H19NO5

SMILES

CC1=C(O)C(C)=C(C)C([C@@]2(C3=CNC4=CC=CC=C43)C(OC)=O)=C1OC2=O

Structure Classification
Initial Source

Umbelopsis sp. DWS 372

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Umbelopsisin A
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HY-179519
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