| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| Targets |
Icariside I targets bone metabolism pathways and cancer-related pathways. It promotes osteoblast differentiation while inhibiting osteoclast formation, helping restore the balance between bone formation and resorption. The compound reverses P-gp-mediated multidrug resistance in cancer cells. It reduces breast cancer proliferation, apoptosis, invasion, and metastasis. Icariside I inhibits the expression of anti-apoptotic proteins Bcl-2 and Bcl-xL. It specifically facilitates ATP or nigericin-induced NLRP3 inflammasome activation.
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| ln Vitro |
In vitro, Icariside I promotes osteoblast differentiation while inhibiting osteoclast formation. It reverses P-gp-mediated multidrug resistance in human MCF7/ADR cells. The compound reduces breast cancer proliferation, apoptosis, invasion, and metastasis. It inhibits the expression of anti-apoptotic proteins Bcl-2 and Bcl-xL. Icariside I specifically facilitates ATP or nigericin-induced NLRP3 inflammasome activation. Its osteogenic and anticancer activities have been characterized in various cell-based assays.
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| ln Vivo |
In vivo, Icariside I shows promising efficacy in preclinical studies for preventing or treating osteoporosis, particularly postmenopausal bone loss. It has been shown to be effective against infectious diseases such as malaria and tuberculosis in mice models. The compound is a metabolite of icariin that regulates bone remodeling. Further in vivo studies have evaluated its bone-protective and anticancer effects.
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| Enzyme Assay |
Icariside I enzyme assays involve measuring its effects on bone metabolism and cancer-related enzymes. Osteoblast differentiation is assessed by measuring alkaline phosphatase activity and mineralization. Osteoclast formation is assessed by TRAP staining. P-gp activity is assessed by measuring efflux of fluorescent substrates. NLRP3 inflammasome activation is assessed by measuring caspase-1 activity and IL-1β release. Bcl-2 and Bcl-xL expression is measured by Western blot. Assays are performed in appropriate buffer systems with positive controls such as known osteogenic agents.
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| Cell Assay |
Icariside I cell-based assays are conducted in osteoblasts, osteoclasts, cancer cell lines, and immune cells. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with Icariside I at varying concentrations. Cell viability is assessed by MTT or CCK-8 assays. Osteoblast differentiation is assessed by alkaline phosphatase staining and mineralization. Osteoclast formation is assessed by TRAP staining. Multidrug resistance reversal is assessed by measuring drug accumulation and cytotoxicity in P-gp-expressing cells. Apoptosis is evaluated by Annexin V/PI staining. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
Icariside I in vivo studies are conducted in animal models of osteoporosis, cancer, and infectious diseases. For osteoporosis studies, ovariectomized mice are treated with Icariside I and bone mineral density is measured by DEXA or micro-CT. For cancer studies, tumor-bearing mice are treated with Icariside I and tumor growth is monitored. For infectious disease studies, mice infected with malaria or tuberculosis are treated with Icariside I and pathogen burden is assessed. Dosing regimens are optimized based on pharmacokinetic data. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biomarker analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Icariside I (MW 530.52 g/mol, C27H30O11) is a flavonoid glycoside. It is an active metabolite of icariin found in Epimedium. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies. Icariside I is used in bone and cancer research.
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| Toxicity/Toxicokinetics |
Icariside I is generally well-tolerated in preclinical studies. The compound is a natural flavonoid glycoside from Epimedium with established safety profiles. Its osteogenic and anticancer activities have been demonstrated with acceptable safety profiles. 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.
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| References |
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| Additional Infomation |
Icariside I has been reported to be found in Epimedium brevicornu, Epimedium truncatum, and other organisms with available data.
Icariside I is a flavonoid glycoside and active metabolite of icariin from Epimedium with osteogenic and anticancer activities. It promotes osteoblast differentiation and inhibits osteoclast formation, showing efficacy in osteoporosis models. The compound reverses P-gp-mediated multidrug resistance and reduces breast cancer proliferation, invasion, and metastasis. Its molecular formula is C27H30O11 with a molecular weight of 530.52 g/mol. All applications are limited to non-human research use. |
| Molecular Formula |
C27H30O11
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|---|---|
| Molecular Weight |
530.5205
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| Exact Mass |
530.178
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| CAS # |
56725-99-6
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| PubChem CID |
5745470
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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 |
801.3±65.0 °C at 760 mmHg
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| Flash Point |
267.8±27.8 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.664
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
892
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC(=CCC1=C(C=C(C2=C1OC(=C(C2=O)O)C3=CC=C(C=C3)OC)O)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)C
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| InChi Key |
IYCPMVXIUPYNHI-WPKKLUCLSA-N
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| InChi Code |
InChI=1S/C27H30O11/c1-12(2)4-9-15-17(36-27-24(34)22(32)20(30)18(11-28)37-27)10-16(29)19-21(31)23(33)25(38-26(15)19)13-5-7-14(35-3)8-6-13/h4-8,10,18,20,22,24,27-30,32-34H,9,11H2,1-3H3/t18-,20-,22+,24-,27-/m1/s1
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| Chemical Name |
3,5-dihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~62.5 mg/mL (~117.81 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (3.92 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 (3.92 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 | 1.8849 mL | 9.4247 mL | 18.8494 mL | |
| 5 mM | 0.3770 mL | 1.8849 mL | 3.7699 mL | |
| 10 mM | 0.1885 mL | 0.9425 mL | 1.8849 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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