Glycycoumarin

SKU: orb1217441

Description

Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.

Key Properties

• CAS Number: 94805-82-0
• MW: 368.37
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₀O₆
• SMILES: O=C1C(C2=CC=C(O)C=C2O)=CC3=C(OC)C(C/C=C(C)\C)=C(O)C=C3O1
• Target: Autophagy
• Solubility: DMSO:Soluble

Bioactivity

• In Vivo:
  Glycycoumarin (30 μM-0.3 nM; 5 min) has an inhibitory effect on smooth muscle contraction induced by various types of stimulants through the inhibition of PDEs, especially isozyme 3, followed by the accumulation of intracellular cAMP. Glycycoumarin (10 mg/kg; i.p.; once daily for 4 d) enhances tumor growth inhibition in HepG2 xenograft model in mice and shows synergistical effect with ABT-737 (HY-50907). Animal model: Male ICR mice (aged 6 weeks, weight 25-30 g). Dosage: 30 μM-0.3 nM, 5 min. Administration:. Result: Inhibited the contraction induced by various types of stimulants, such as CCh, KCI, BaCI(2), and A23187 (calcium ionophore III). Enhanced the relaxation induced by forskolin on CCh-evoked contraction and also enhances the relaxation effect of rolipram. Associated with dose-dependent accumulation of cAMP. Animal model: HepG2 cancer cells xenograft model in male BALB/c athymic nude mice (6-7 weeks old). Dosage: 10 mg/kg. Administration: Intraperitoneal injection; once daily for 4 days; ABT-737 group was given 100 mg/kg i.p. Result: Inhibited tumor growth and resulted a reduction of the final tumor weight by 17%.
• In Vitro:
  Glycycoumarin, (25 μM; 24 h) combining with ABT-737 (12.5 μM) synergistically, induces cell death in multiple types of liver cancer cell HepG2.Glycycoumarin is highly effective against alcoholic liver disease, nonalcoholic fatty liver disease, acetaminophen-induced hepatotoxicity, and liver cancer through mechanisms involved in activation of Nrf2 antioxidant system, stimulation of AMPK-mediated energy homeostasis, induction of autophagy degradation process, and inhibiting oncogenic kinase T-lymphokine-activated killer cell-originated protein kinase activity. Cell Viability Assay Cell line: HepG2, SMMC-7721, and Huh-7. Concentration: 10, 20, 25, 30, and 40 μM. Incubation time: 24 hours. Result: Induced cell death in multiple types of liver cancer cell lines in a dose-dependent manner.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Autophagy