Lunularin is an inhibitor of 11beta-hydroxysteroid dehydrogenase 1, with an IC50 of 45.44 µM and a Ki of 35.8 µM against human 11beta-HSD1, and an IC50 of 17.39 µM and a Ki of 10.31 µM against rat 11beta-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-kappaB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11beta-HSD1 and the steroid/NADPH-binding region of rat 11beta-HSD1, but does not inhibit 11beta-HSD2 or mouse 11beta-HSD1. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome[1][2][3][4].
Molecular Weight:
214.26
Purity:
99.87
CAS Number:
[37116-80-6]
Formula:
C14H14O2
Target:
11beta-HSD,Endogenous Metabolite
Application Notes:
MCE Product type: Reference compound
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