| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Oroxylin A targets multiple pathways including IL-6/STAT3, NF-κB, CDK9, MDM2, and SIRT1. It inhibits the phosphorylation of MDM2 and SIRT1 through CDK9 inhibition, thus inhibiting MDM2-mediated degradation of P53 and SIRT1-mediated deacetylation of P53, ultimately stabilizing the P53 protein. The compound acts as a transketolase (TKT) inhibitor with a SPR KD of 70.7 μM. It inhibits the activation of hepatic stellate cells by inhibiting SIRT7. Oroxylin A also modulates drug resistance by targeting efflux pump genes.
|
|---|---|
| ln Vitro |
Oroxylin A (20 μM; 24 hours) prevents MDA-MB-231 cells from proliferating, growing, and migrating. Moreover, oroxylin A can prevent MDA-MB-231 from invading and from going through the epithelial-mesenchymal transition (EMT) pathway [4]. Moreover, oroxylin A (20 μM; 24 h) suppresses the NF-κB signaling pathway and pro-inflammatory cytokine expression [4]. TNF-α neutralizes the anti-inflammatory properties of oroxylin A [4].
In vitro, Oroxylin A demonstrates strong anticancer activity against various cancer cell lines. It inhibits the IL-6/STAT3 pathway and NF-κB signaling, inhibiting cell proliferation and inducing apoptosis. The compound inhibits hepatocellular carcinoma growth in vitro. It functions as a dopamine reuptake inhibitor. Oroxylin A has been shown to modulate drug resistance by targeting efflux pump genes, reducing the expulsion of therapeutic agents from cells. Its effects on immune response modulation have also been reported. |
| ln Vivo |
In vivo, Oroxylin A inhibits hepatocellular carcinoma growth. It has been found to improve memory consolidation in mice by elevating brain-derived neurotrophic factor (BDNF). The compound modulates drug resistance by targeting efflux pump genes. It may enhance immune system responses, contributing to improved antiviral defenses. Oroxylin A has been studied in various animal models for its anti-cancer, neuroprotective, and immunomodulatory effects. Further in vivo studies are ongoing to fully characterize its therapeutic potential.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Oroxylin A include transketolase inhibition studies with SPR KD determination of 70.7 μM. GABAA receptor binding assays assess negative allosteric modulation of the benzodiazepine site. Dopamine reuptake inhibition is measured using synaptosomal preparations or cells expressing dopamine transporters. CDK9 kinase activity assays are performed to assess inhibition of MDM2 and SIRT1 phosphorylation. NF-κB DNA binding assays and STAT3 phosphorylation studies are conducted to evaluate pathway inhibition. Assays are performed in appropriate buffer systems with positive controls.
|
| Cell Assay |
In vitro cell-based assays for Oroxylin A are conducted in various cancer cell lines including hepatocellular carcinoma cells. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with Oroxylin A at varying concentrations. Cell viability is assessed by MTT or CCK-8 assays. Apoptosis is evaluated by Annexin V/PI staining and caspase activity assays. P53 protein levels and phosphorylation status are analyzed by Western blot. IL-6/STAT3 and NF-κB pathway activation is assessed by Western blot or reporter gene assays. Experiments are performed in triplicate with appropriate controls.
|
| Animal Protocol |
In vivo animal studies for Oroxylin A are conducted in mouse models of hepatocellular carcinoma and other cancers. Tumor-bearing mice are treated with Oroxylin A via oral administration or intraperitoneal injection. Tumor growth is monitored by caliper measurements. For memory studies, mice are treated with Oroxylin A and assessed in behavioral tests such as Morris water maze. BDNF levels in brain tissues are measured by ELISA or Western blot. For immunomodulation studies, animal models of infection or immune challenge are used. Dosing regimens are optimized based on pharmacokinetic data.
|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
The known human metabolites of Oroxylin A include (2S,3S,4S,5R)-3,4,5-trihydroxy-6-(5-hydroxy-6-methoxy-4-oxo-2-phenylchromene-7-yl)oxaoxane-2-carboxylic acid. Oroxylin A (MW 284.27 g/mol, C16H12O5) is a flavonoid with favorable drug-like properties. The compound is an O-methylated flavone with good oral bioavailability as demonstrated by its efficacy in oral administration studies. Oroxylin A is metabolized by hepatic enzymes. The compound is distributed to tissues including brain, as evidenced by its effects on memory consolidation and BDNF elevation. Pharmacokinetic parameters such as Cmax, Tmax, and half-life would be determined in species-specific studies. The compound shows stability under recommended storage conditions. |
| Toxicity/Toxicokinetics |
Oroxylin A is generally well-tolerated in preclinical studies at therapeutic doses. The compound is a natural flavonoid derived from Scutellaria baicalensis and Oroxylum indicum, plants used in traditional medicine. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
|
| References |
|
| Additional Infomation |
Oroxylin A is a dihydroxy monomethoxyflavonoid with hydroxyl groups at C-5 and C-7 positions and a methoxy group at C-6 position. It possesses antitumor activity and is also an EC 1.14.13.39 (nitric oxide synthase) inhibitor. It is both a monomethoxyflavonoid and a dihydroxyflavonoid. It is the conjugate acid of Oroxylin A(1-). Oroxylin A has been reported to be found in Rhinacanthus nasutus, Scutellaria racemosa, and other organisms with relevant data.
Oroxylin A is an O-methylated flavone found in Scutellaria baicalensis and Oroxylum indicum. It has strong anti-cancer effects through inhibition of IL-6/STAT3 and NF-κB pathways. The compound inhibits CDK9, leading to P53 stabilization. Oroxylin A functions as a dopamine reuptake inhibitor and a negative allosteric modulator of the GABAA receptor. It inhibits transketolase with a KD of 70.7 μM. The compound improves memory consolidation in mice by elevating BDNF. All applications are limited to non-human research use. |
| Molecular Formula |
C₁₆H₁₂O₅
|
|---|---|
| Molecular Weight |
284.26
|
| Exact Mass |
284.068
|
| CAS # |
480-11-5
|
| PubChem CID |
5320315
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
540.9±50.0 °C at 760 mmHg
|
| Melting Point |
195-197ºC
|
| Flash Point |
207.4±23.6 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.669
|
| LogP |
2.37
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
21
|
| Complexity |
426
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LKOJGSWUMISDOF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H12O5/c1-20-16-11(18)8-13-14(15(16)19)10(17)7-12(21-13)9-5-3-2-4-6-9/h2-8,18-19H,1H3
|
| Chemical Name |
5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one
|
| Synonyms |
Baicalein 6-methyl etherOroxylin A
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 32 mg/mL (~112.57 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5179 mL | 17.5895 mL | 35.1791 mL | |
| 5 mM | 0.7036 mL | 3.5179 mL | 7.0358 mL | |
| 10 mM | 0.3518 mL | 1.7590 mL | 3.5179 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
