Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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Other Sizes |
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Purity: ≥98%
Baicalein (5,6,7-Trihydroxyflavone; Noroxylin; BaiKalein), a naturally occuring flavone, is a potent inhibitor of CYP2C9, prolyl endopeptidase, and xanthine oxidase with important biological activity (e.g, antioxidant, anti-inflammation, antifibrotic). Baicalin can be isolated from several species in the genus Scutellaria, including Scutellaria lateriflora (blue skullcap). There are 10 mg/g baicalin in Scutellaria galericulata (common skullcap) leaves. Baicalin is the glucuronide of baicalein. It is a component of Chinese medicinal herb Huang-chin (Scutellaria baicalensis) and one of the chemical ingredients of Sho-Saiko-To, an herbal supplement. Baicalin is a known prolyl endopeptidase inhibitor, induces apoptosis in pancreatic cancer cells, and affects the GABA receptors.
ln Vitro |
In vitro, baicalein suppresses the proliferation and cytokine release of T cells stimulated by mitogens. Pretreatment with Baicalein at 25 μM dramatically reduced the amount of proliferation and cytokine production that Con A or anti-CD3/CD28 mAb could cause. Treatment with baicalein causes NF-κB to bind to DNA, but it also prevents the nuclear compartment's thioredoxin activity from occurring [2]. Baicalein has a dose- and time-dependent inhibition on the proliferation, migration, and invasion of MDA-MB-231 cells. In MDA-MB-231 cells, baicalein dramatically lowered the expression of SATB1. Baicalein also reduces the transcription levels of genes targeted by Wnt/β-catenin, as well as the production of Wnt1 and β-catenin proteins [3].
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ln Vivo |
Baicalein prevents the development of graft-versus-host disease, but it has no effect on the mouse T cell population's homeostatic growth. This finding unequivocally shows that baicalein has strong in vivo anti-inflammatory properties [2]. Interventricular septal thickness, brain natriuretic peptide plasma levels, left ventricular myocardial collagen volume, and heart-to-body weight ratio all increased less in rats given baicalein treatment (P < 0.05, respectively). The suppression of left ventricular procollagen I and III expression, along with decreased expression of 12-lipoxygenase, matrix metallopeptidase 9 expression and activity, and extracellular signal-regulated kinase activity, all contribute to the anti-fibrotic effect of baicalein. In hypertensive rats, baicalein can prevent myocardium fibrosis [4].
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Animal Protocol |
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References |
[1]. Shieh DE,et al. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res. 2000 Sep-Oct;20(5A):2861-5.
[2]. Patwardhan RS, et al. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation. Biochem Pharmacol. 2016 May 15;108:75-89. [3]. Ma X, et al. Baicalein suppresses metastasis of breast cancer cells by inhibiting EMT via downregulation of SATB1 and Wnt/β-catenin pathway. Drug Des Devel Ther. 2016 Apr 18;10:1419-41. [4]. Kong EK, et al. A novel anti-fibrotic agent, baicalein, for the treatment of myocardial fibrosis in spontaneously hypertensiverats. Eur J Pharmacol. 2011 May 11;658(2-3):175-81 |
Molecular Formula |
C15H10O5
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Molecular Weight |
270.24
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CAS # |
491-67-8
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Related CAS # |
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SMILES |
O1C(C2C([H])=C([H])C([H])=C([H])C=2[H])=C([H])C(C2C(=C(C(=C([H])C1=2)O[H])O[H])O[H])=O
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InChi Key |
FXNFHKRTJBSTCS-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H10O5/c16-9-6-11(8-4-2-1-3-5-8)20-12-7-10(17)14(18)15(19)13(9)12/h1-7,17-19H
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Chemical Name |
5,6,7-Trihydroxy-2-phenylchromen-4-one
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.25 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (9.25 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 20 mg/mL (74.01 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.7004 mL | 18.5021 mL | 37.0041 mL | |
5 mM | 0.7401 mL | 3.7004 mL | 7.4008 mL | |
10 mM | 0.3700 mL | 1.8502 mL | 3.7004 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03830684 | Unknown † | Drug: Baicalein Tablets 400mg Drug: Baicalein Tablets 600mg |
Influenza | CSPC ZhongQi Pharmaceutical Technology Co., Ltd. |
February 1, 2019 | Phase 2 |
Baicalein inhibits the motility of MDA-MB-231 cells. Notes: (A) Monolayers of MDA-MB-231 cells were wounded and then incubated in media containing 2% FBS with varying concentrations of baicalein (0, 10, 20, and 40 μmol/L) for 24 hours. Pictures were taken at 0, 12, and 24 hours after addition of baicalein. (B) Quantification of the wound healing assay. *P<0.05 compared with control; **P<0.01 compared with control. Data are presented as the mean ± SD of three separate experiments. Abbreviations: FBS, fetal bovine serum; SD, standard deviation; h, hours. td> |
Baicalein inhibits the invasiveness of MDA-MB-231 cells. Notes: (A) MDA-MB-231 cells were pretreated with 0, 10, 20, and 40 μmol/L baicalein for 24 hours and were then seeded in the upper wells. FBS (10%) was added to the bottom chambers for 24 hours to induce cell invasion. After 24 hours, cells on the bottom side of the filter were fixed, stained, and counted. (B) The percent invasion rate was expressed as a percentage of the control (0 μmol/L). Values represent the mean ± SD of three independent experiments performed in triplicate. **P<0.01 compared with control group. Abbreviations: FBS, fetal bovine serum; SD, standard deviation. td> |
Baicalein suppresses liver metastasis of breast cancer in vivo. Notes: Macroscopic findings of liver metastasis in the control group (A) and the high-dose prevention group (B). Microscopic findings of liver metastases in control group (C) and hardly seen metastatic lesions in high-dose prevention group (D). The black arrows show the lung metastases in each group, magnification of 100×. td> |