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Umbelliferone (7-Hydroxycoumarin), a natural orally active product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent. Umbelliferone induces cell cycle arrest, apoptosis and DNA fragmentation in HepG2 cells. Umbelliferone exhibits significant anticancer effects. Umbelliferone attenuates the alteration characteristics of allergic airway inflammation. Umbelliferone displays the neuroprotective effects and cross the blood-brain barrier. Umbelliferone exhibits anti-inflammatory and antioxidant effects in
chronic alcohol-fed rats.
For research use only. We do not sell to patients.
Umbelliferone (7-Hydroxycoumarin), a natural orally active product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent. Umbelliferone induces cell cycle arrest, apoptosis and DNA fragmentation in HepG2 cells. Umbelliferone exhibits significant anticancer effects. Umbelliferone attenuates the alteration characteristics of allergic airway inflammation. Umbelliferone displays the neuroprotective effects and cross the blood-brain barrier. Umbelliferone exhibits anti-inflammatory and antioxidant effects in
chronic alcohol-fed rats[1][2][3][4].
IC50 & Target
Human Endogenous Metabolite
Cellular Effect
Cell Line
Type
Value
Description
References
A549
IC50
> 100 μM
Compound: 6
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Anticancer activity against human SK-MEL3 cells assessed as reduction in cell viability incubated for 24 hrs in presence of Artesunic acid by MTT assay
Anticancer activity against human SK-MEL3 cells assessed as reduction in cell viability incubated for 24 hrs in presence of Artesunic acid by MTT assay
Umbelliferone (1-50 μM, 12-48 h) induces a dose‑dependent and time‑dependent reduction in HepG2 cells viability[1].
Umbelliferone (0-50 μM, 24 h) results in the appearance of HepG2 cell shrinkage, membrane blebbing, nuclear condensation and apoptotic body formation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Resulted in the appearance of cell shrinkage and membrane blebbing, when compared with the morphology of untreated cells.
At 50 μM almost all the HepG2 cancer cells shrank significantly and no cells with normal morphological features were detected.
Reduced large nuclei.
Induced nuclear condensation and apoptotic body formation.
Increased in the proportion of cells in S phase (45.0, 51.3 and 62.1%, compared with 43.6% in untreated cells) and reduced in the fraction of cells in G1 phase (42.1, 45.6 and 32.2%, compared with 53.2% in the untreated cells).
In Vivo
Umbelliferone (90 mg/kg, p.o., daily, 5 days) reduces the number of total cells, neutrophils, eosinophils and mononuclear cells in the bronchoalveolar lavage fluid of challenged mice[2].
Umbelliferone (15-30 mg/kg, i.g., daily, 21 days) shows neuroprotective effects on CUMS (chronic unpredictable mild stress)-induced rat model of depression, which is associated with the inhibition of neuronal apoptosis modulated by ROCK/Akt pathway[3].
Umbelliferone (0.05 g/L, p.o., daily, 8 weeks) protects against alcohol-induced liver damage by inhibiting the TLR4 signaling pathway and activating the antioxidant system in rats with liber-decarli liquid diet containing 5% alcohol [4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male BALB/c mice, 4-6 weeks old received systemic immunization by subcutaneous injection of 10 μg of chicken egg ovalbumin diluted in 2 mg/mL alum followed by a booster injection at day 14. A nasal challenge was performed starting at day 28, by inhalational exposure to aerosolised ovalbumin for 15 min/day, on five consecutive days[2].
Dosage:
30, 60, 90 mg/kg
Administration:
p.o., daily, 5 days
Result:
Mice sensitized and challenged with ovalbumin have increased the number of inflammatory cells in bronchoalveolar lavage fluid.
Reduced the number of total cells and of neutrophils in the bronchoalveolar lavage fluid.
At 60 and 90 mg/kg, but not at 30 mg/kg, decreased significantly the number of eosinophils found in the bronchoalveolar lavage fluid of challenged mice.
At 60 mg/kg, decreased the number of mononuclear cells.
Caused a reduction in the levels of Th2-associated cytokines (IL-4, IL-5, IL-13).
Animal Model:
While the control group of rats without receiving stress treatment had free access to food and water, other groups of rats were subjected to different types of stressors: cage tilting for 24 h, damp sawdust for 24 h, predator sounds, swimming in 4 ℃ cold water for 5min, swimming in 45 ℃ hot water for 5min, fasting for 48 h, water deprivation for 24 h, shaking for 15 min, nip trail for 1 min[3][5].
Dosage:
15,30 mg/kg
Administration:
i.g., daily, 21 days
Result:
Exhibited an antidepressant-like effect, as sucrose consumption in CUMS rats significantly increased.
Decreased the expression of caspase3 and bax and increased the expression of bcl2 in CA1 region of hippocampus compared to the control group.
Remarkably increased the number of nissl-positive cells.
Down-regulated the levels of inflammatory cytokines IL-1β, IL-6 and TNF-α in hippocampus in the CUMS group versus control group.
Decreased the protein level of ROCK2 and phosphorylation expression of PTEN stimulated by CUMS.
Up-regulated the phosphorylation expressions of Akt and GSK3.
Animal Model:
Rats were fed a Liber-Decarli liquid diet containing 5% alcohol for 8 weeks, while normal rats received an isocaloric carbohydrate liquid diet[4].
Dosage:
0.05 g/L
Administration:
p.o., daily, 8 weeks
Result:
Decreased in serum TNF-α and IL-6 levels and increased IL-10 level.
Decreased the mRNA expressions of LBP, TLR4, NF-κB and TNF-α and IL-6.
Up-regulated SOD and CAT mRNA levels and activity.
Increased H2O2 and GSH levels and decreased hepatic MDA (Malondialdehyde) levels.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (616.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
6.1674 mL
30.8368 mL
61.6736 mL
5 mM
1.2335 mL
6.1674 mL
12.3347 mL
10 mM
0.6167 mL
3.0837 mL
6.1674 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Solubility: 1.43 mg/mL (8.82 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1.43 mg/mL.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.43 mg/mL (8.82 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1.43 mg/mL.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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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