Baicalein
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Catalog No.GN10158
One-Click Copy Product Info
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Baicalein (5,6,7-trihydroxyflavone) is a flavonoid compound with multiple biological activities. It is a xanthine oxidase inhibitor with an IC50 value of 3.12μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 491-67-8
Sample solution is provided at 25 µL, 10mM.
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Baicalein (5,6,7-trihydroxyflavone) is a flavonoid compound with multiple biological activities. It is a xanthine oxidase inhibitor with an IC50 value of 3.12μM[1]. Baicalein interacts with the benzodiazepine binding site of the GABAA receptor in mouse cortical membrane preparations with a Ki value of 13.1μM[2]. Baicalein has anti-tumor and anti-inflammatory activities, and can also play a neuroprotective and mitochondrial protective role[3].
In vitro, Baicalein (25μM) treatment of mouse spleen lymphocytes for 2h significantly inhibited mitogen-induced T cell proliferation and cytokine secretion, and also inhibited the upregulation of CD69 and CD25 (IL2Rα), but did not inhibit CD54 (ICAM-1) expression[4]. Baicalein (0-160 μM) was treated for 24 h in two ovarian cancer (OVCAR-3 and CP-70) cell lines and one normal ovarian cell line (IOSE-364), selectively inhibiting cancer cell viability, while the inhibitory effect on normal ovarian cells was significantly less. It also inhibited the expression of oncogenes such as VEGF, HIF-1α, cMyc and NFκB[5].
In vivo, Baicalein (1, 3 mg/kg) was treated by intratumoral injection in mice inoculated with H-460 tumor cells for 4 weeks, which significantly inhibited tumor growth, reduced the expression of 12-LOX and VEGF in tumor tissue, and reduced the mitotic cell index and microvascular density[6]. Baicalein (30, 100 mg/kg) was used to treat mice with acidified ethanol-induced acute gastric ulcers, significantly inhibited the formation of acute ulcers, reduced the inflammatory process, stimulated cellular antioxidant mechanisms, and increased gastric mucus secretion[7].
References:
[1] Shieh D, Liu L T, Lin C C. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin[J]. Anticancer research, 2000, 20(5A): 2861-2865.
[2] Liao J F, Hung W Y, Chen C F. Anxiolytic-like effects of baicalein and baicalin in the Vogel conflict test in mice[J]. European journal of pharmacology, 2003, 464(2-3): 141-146.
[3] De Oliveira M R, Nabavi S F, Habtemariam S, et al. The effects of baicalein and baicalin on mitochondrial function and dynamics: A review[J]. Pharmacological Research, 2015, 100: 296-308.
[4] Patwardhan R S, Sharma D, Thoh M, et al. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation[J]. Biochemical Pharmacology, 2016, 108: 75-89.
[5] Chen J, Li Z, Chen A Y, et al. Inhibitory effect of baicalin and baicalein on ovarian cancer cells[J]. International journal of molecular sciences, 2013, 14(3): 6012-6025.
[6] Cathcart M C, Useckaite Z, Drakeford C, et al. Anti-cancer effects of baicalein in non-small cell lung cancer in-vitro and in-vivo[J]. BMC cancer, 2016, 16: 1-13.
[7] Ribeiro A R S, do Nascimento Valença J D, da Silva Santos J, et al. The effects of baicalein on gastric mucosal ulcerations in mice: Protective pathways and anti-secretory mechanisms[J]. Chemico-Biological Interactions, 2016, 260: 33-41.
| Cell experiment [1]: | |
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Cell lines |
Murine splenic lymphocytes |
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Preparation Method |
CFSE stained murine splenic lymphocytes were pre-treated with 5 to 25µM of Baicalein for 2 h and stimulated with Con A (T-cell mitogen) or anti-CD3/CD28 mAb and proliferation was assessed by CFSE dye dilution using a flow cytometer. |
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Reaction Conditions |
5-25μM; 2h |
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Applications |
Pre-treatment with 25µM Baicalein significantly suppressed Con A or anti-CD3/CD28 mAb induced proliferation as well as cytokine secretion. |
| Animal experiment [2]: | |
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Animal models |
Male nude mice |
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Preparation Method |
H-460 cells were administered subcutaneously into the left dorsal flank of 6-week-old male nude mice (BALBc). When tumour size reached approximately 50 mm3, animals were randomised into control and treatment groups. Mice were administered Baicalein (1 mg/kg or 3 mg/kg in 50μl DMSO/PBS), or an equal volume of a vehicle control, by intratumoural injection. Intratumoural injection was carried out twice weekly, and tumour size was measured every 48 h using a digital callipers. |
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Dosage form |
1, 3mg/kg; intratumoural injection |
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Applications |
Baicalein-treated H-460 tumors showed significantly reduced growth, decreased 12-LOX and VEGF expressions, and significantly decreased mitotic cell index and microvessel density. |
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References: |
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| Cas No. | 491-67-8 | SDF | |
| Chemical Name | 5,6,7-trihydroxy-2-phenylchromen-4-one | ||
| Canonical SMILES | C1=CC=C(C=C1)C2=CC(=O)C3=C(C(=C(C=C3O2)O)O)O | ||
| Formula | C15H10O5 | M.Wt | 270.24 |
| Solubility | ≥ 10.9mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7004 mL | 18.5021 mL | 37.0041 mL |
| 5 mM | 740.1 μL | 3.7004 mL | 7.4008 mL |
| 10 mM | 370 μL | 1.8502 mL | 3.7004 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)