Diosmetin

SKU: orb1307680

Description

Diosmetin, a methylated derivative of luteolin, exhibits weak agonist activity at the TrkB receptor. This small molecule is utilized in neuroscience research to study neurotrophic signaling pathways in both cellular and animal models of neuronal survival and plasticity.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 520-34-3
• MW: 300.26
• Purity: 99.59%
• Formula: C₁₆H₁₂O₆
• SMILES: O=C1C=2C(OC(=C1)C3=CC(O)=C(OC)C=C3)=CC(O)=CC2O
• Target: Trk receptor,Cytochromes P450
• Solubility: DMSO:39 mg/mL (129.89 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.66 mM)

Bioactivity

• Target IC50:
  CYP1A enzyme(human, HepG2 cells):40 μM
• In Vivo:
  After 6 h, 9 h, 12 h of the first cerulein injection, the severity of acute pancreatitis was evaluated biochemically and morphologically. Pretreatment with diosmetin significantly reduced serum levels of amylase and lipase; the histological injury; the secretion of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6; myeloperoxidase (MPO) activity, trypsinogen activation peptide (TAP) level, the expression of inducible nitric oxide synthase (iNOS); and the nuclear factor (NF)-κB activation in cerulein-induced AP. This study showed that administration of diosmetin demonstrated a beneficial effect on the course of cerulein-induced AP in mice. Therefore, diosmetin may become a new therapeutic agent in future clinical trials for treatment of AP.
• Cell Research:
  Diosmetin is dissolved in DMSO which is maintained at a constant concentration in control samples (2%). HepG2 cells are maintained in a humidified atmosphere of 5% CO2 at 37°C, and cultured in RPMI-1640 medium supplemented with 10% (v/v) fetal bovine serum, 100 U/mL penicillin and 100 U/mL streptomycin. HepG2 cell density is adjusted to 2×104 cells/100 μL, and the cells are seeded into 96-well plates and placed in an incubator overnight (37°C in 5% CO2) to allow for attachment and recovery. MTT analyses are performed. Briefly, cells are pretreated with 5, 10, 15 and 20 μg/mL diosmetin for 24 h. A total of 20 μL MTT solution (5 mg/mL in PBS) solution is transferred to each well to yield a final 120 μL/well and to separate wells a total of 10 μL CCK8 (5 mg/mL in PBS) is transferred. The plates are incubated for 4 h at 37°C in 5% CO2 and the absorbance is recorded at wavelengths of 595 nm and 450 nm, respectively. The half maximal inhibitory concentration (IC50) of diosmetin is calculated.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Trkreceptor, TrkB, Trk receptor, Inhibitor, inhibit, Luteolin 4-methyl ether, Cytochrome P450, CYP1A1, CYPs, Diosmetin

Compound Identifiers

PubChem CID

5281612