| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Noricaritin targets estrogen receptor alpha (ERα) with high affinity (Ki = 55 nM), while its activity at ERβ is significantly lower (Ki ≈ 6.05 μM), suggesting a distinct ER subtype selectivity profile. The compound also modulates gene expression, inhibits inflammatory mediators, induces apoptosis, and regulates cell proliferation and differentiation. Its anti-inflammatory activity involves inhibition of pro-inflammatory cytokine and chemokine production in epithelial cells.
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| ln Vitro |
Noricaritin has demonstrated significant in vitro activity as an anti-inflammatory, antioxidant, anticancer, and neuroprotective agent. In human lung epithelial cells, it inhibits the production of pro-inflammatory cytokines and chemokines. Noricaritin induces cell proliferation in lung tissue. It has been shown to regulate gene expression, inhibit inflammatory mediators, induce apoptosis, and modulate cell proliferation and differentiation. The compound exhibits high affinity for ERα (Ki = 55 nM) with significant selectivity over ERβ.
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| ln Vivo |
In vivo studies have demonstrated Noricaritin's therapeutic potential for autoimmune diseases, bone growth, and the prevention of heat-shock protein denaturation. The compound shows anti-inflammatory, antimicrobial, and anticancer effects in various experimental models. Its ability to modulate gene expression and inhibit inflammatory mediators translates to in vivo anti-inflammatory activity. The compound has been studied for its effects on bone growth and immune system modulation. Further in vivo studies are needed to fully characterize its pharmacokinetic and pharmacodynamic profile.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for Noricaritin typically involve radioligand binding studies for estrogen receptors. ERα and ERβ proteins are expressed in recombinant systems and incubated with increasing concentrations of Noricaritin (0.1 nM - 10 μM) and a fixed concentration of radiolabeled estradiol (e.g., ³H-estradiol, 0.5-1 nM) in binding buffer at 4°C for 16-24 hours. Bound and free radioligand are separated by charcoal-dextran precipitation or filtration through glass fiber filters. Radioactivity is measured by liquid scintillation counting. IC₅₀ values are determined by nonlinear regression, and Ki values are calculated using the Cheng-Prusoff equation. Specific binding is defined as total binding minus non-specific binding in the presence of excess unlabeled estradiol.
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| Cell Assay |
For in vitro cell-based assays, human lung epithelial cells or other relevant cell lines are cultured in appropriate media supplemented with fetal bovine serum and antibiotics. Cells are treated with Noricaritin at concentrations ranging from 1-100 μM for 24-72 hours. Cell proliferation is assessed by MTT, CCK-8, or BrdU incorporation assays. For anti-inflammatory studies, cells are stimulated with pro-inflammatory agents (e.g., LPS, TNF-α) with or without compound pretreatment. Cytokine and chemokine levels (IL-6, IL-8, TNF-α) in culture supernatants are measured by ELISA. Apoptosis is evaluated by Annexin V-FITC/PI staining and caspase activity assays. Gene expression changes are analyzed by qRT-PCR and Western blot.
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| Animal Protocol |
In vivo animal studies with Noricaritin typically use rodent models for various disease indications. For anti-inflammatory studies, mice are administered Noricaritin orally or intraperitoneally at doses ranging from 5-50 mg/kg daily for 7-14 days, followed by induction of inflammation (e.g., carrageenan-induced paw edema, LPS-induced lung inflammation). Inflammatory markers in serum and tissues are measured by ELISA. For bone growth studies, ovariectomized rat models are used to assess the compound's effects on bone density and turnover. For anticancer studies, xenograft tumor models are established in immunodeficient mice, and tumor growth is monitored following compound administration. Tissue samples are collected for histopathological and molecular analyses.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Noricaritin are characteristic of flavonoid compounds. Following oral administration, flavonoids typically have moderate to low bioavailability due to extensive first-pass metabolism, including glucuronidation and sulfation in the intestine and liver. The compound has a molecular weight of 372.37 g/mol and is soluble in DMSO, chloroform, dichloromethane, ethyl acetate, and acetone. Storage recommendations are powder at -20°C for 3 years and in solvent at -80°C for 1 year. Tissue distribution and elimination half-life data are limited for this specific compound.
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| Toxicity/Toxicokinetics |
Noricaritin is considered to have a favorable safety profile as a natural flavonoid compound. In preclinical studies, the compound has shown no significant toxicity at pharmacologically relevant doses. As a component of Epimedium extracts, which have a long history of traditional use, the compound is generally well-tolerated. However, high doses may cause gastrointestinal effects. No specific toxicity data are available for Noricaritin alone. The compound has demonstrated anti-inflammatory and antioxidant activities that may provide protective effects against oxidative stress-induced damage.
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| Additional Infomation |
Reports have indicated that Phellodendron bark contains norscarin, and relevant data is available for reference.
Noricaritin is a natural flavonoid derived from the roots of Epimedium brevicornu Maxim, a plant widely used in traditional Chinese medicine. It has been studied for its therapeutic effects on autoimmune diseases, bone growth, and the prevention of heat-shock protein denaturation. The compound shows promise in cancer research, cardiovascular health, and neurological studies. Its distinct ER subtype selectivity (ERα vs. ERβ) makes it a valuable tool for studying estrogen receptor biology. Noricaritin is not approved as a therapeutic drug and is intended for research purposes only. |
| Molecular Formula |
C20H20O7
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|---|---|
| Molecular Weight |
372.3686
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| Exact Mass |
372.12
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| CAS # |
5240-95-9
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| PubChem CID |
14427423
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
650.2±55.0 °C at 760 mmHg
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| Flash Point |
234.1±25.0 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.700
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| LogP |
2.41
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
591
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CTGVBHDTGZUEJZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H20O7/c1-20(2,26)8-7-12-13(22)9-14(23)15-16(24)17(25)18(27-19(12)15)10-3-5-11(21)6-4-10/h3-6,9,21-23,25-26H,7-8H2,1-2H3
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| Chemical Name |
3,5,7-trihydroxy-8-(3-hydroxy-3-methylbutyl)-2-(4-hydroxyphenyl)chromen-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~16.67 mg/mL (~44.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.59 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: 2.08 mg/mL (5.59 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6855 mL | 13.4275 mL | 26.8550 mL | |
| 5 mM | 0.5371 mL | 2.6855 mL | 5.3710 mL | |
| 10 mM | 0.2686 mL | 1.3428 mL | 2.6855 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.
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