| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Icariside D2 targets cancer cells through the AKT signaling pathway. It induces apoptosis via alteration of expression of apoptosis-related proteins and decreased phosphorylation of AKT in HL-60 cells. The compound also exhibits anti-inflammatory and anti-HIV activity. As a flavonoid glycoside, Icariside D2 modulates multiple signaling pathways involved in cell survival, proliferation, and inflammation. It is an active metabolite of icariin.
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| ln Vitro |
In HL-60 cells, Icariside D2 3 causes death via changing the expression of proteins linked to apoptosis and lowering AKT phosphorylation[1]. Icariside D2 has anti-HIV and anti-inflammatory properties[3].
In vitro, Icariside D2 shows significant cytotoxic activity on the HL-60 cell line with an IC50 value of 9.0 ± 1.0 µM. It induces apoptosis via alteration of expression of apoptosis-related proteins and decreased phosphorylation of AKT in HL-60 cells. The compound also exhibits anti-inflammatory and anti-HIV activity. These in vitro activities support its potential as an anticancer, anti-inflammatory, and antiviral agent. |
| ln Vivo |
In vivo data for Icariside D2 is limited in publicly available sources. As a natural flavonoid glycoside with cytotoxic activity against HL-60 cells in vitro, the compound is expected to have potential applications in animal models of cancer and inflammation. However, specific published in vivo efficacy studies are not widely reported. Icariside D2 is primarily used as a research compound for studying apoptosis, AKT signaling, and natural product pharmacology.
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| Enzyme Assay |
The in vitro cytotoxicity assay for Icariside D2 is conducted in HL-60 human leukemia cells. Cells are treated with varying concentrations of the compound for 24-72 hours. Cell viability is measured using standard assays such as MTT, and IC50 values are calculated from dose-response curves. Apoptosis is assessed by flow cytometry using Annexin V/PI staining, caspase activity assays, and detection of DNA fragmentation. AKT phosphorylation is measured by Western blotting.
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| Cell Assay |
Cellular assays for Icariside D2 are conducted in HL-60 cells and other cancer cell lines. Cells are treated with varying concentrations of Icariside D2 for 24-72 hours. Cell viability and proliferation are measured using standard assays. Apoptosis is assessed by flow cytometry, caspase activity, and DNA fragmentation. AKT phosphorylation and expression of apoptosis-related proteins are evaluated by Western blotting. Anti-HIV activity is assessed in HIV-infected cell models.
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| Animal Protocol |
In vivo studies for Icariside D2 would typically involve xenograft mouse models of leukemia or other cancers. The compound would be administered via intraperitoneal or oral routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring tumor growth inhibition, with pharmacodynamic markers such as apoptosis and AKT phosphorylation evaluated in tumor tissues. However, specific published in vivo protocols for Icariside D2 are not available in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Icariside D2 is not extensively reported in publicly available sources. The compound has a molecular weight of 300.30 g/mol and a molecular formula of C14H20O7. Storage conditions: 2-8°C. As a flavonoid glycoside, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life and bioavailability are not available in the current literature for this research compound.
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| Toxicity/Toxicokinetics |
Toxicity data for Icariside D2 is limited in publicly available sources. As with all research compounds, Icariside D2 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment. The compound's natural origin suggests a potential safety profile, but comprehensive toxicology studies have not been reported.
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| References |
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| Additional Infomation |
Icariside D2 is a glycoside. It has been reported that Icariside D2 is found in Schisandra chinensis, Rhodiola rosea, and other organisms with relevant data.
Icariside D2 is a natural flavonoid glycoside isolated from Annona glabra and Epimedium species. It shows significant cytotoxic activity on the HL-60 cell line with an IC50 of 9.0 ± 1.0 µM. It induces apoptosis via decreased phosphorylation of AKT in HL-60 cells. Icariside D2 also exhibits anti-inflammatory and anti-HIV activity. It has a molecular formula of C14H20O7 and a molecular weight of 300.30 g/mol. Icariside D2 is an active metabolite of icariin. |
| Molecular Formula |
C14H20O7
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|---|---|
| Molecular Weight |
300.30
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| Exact Mass |
300.121
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| CAS # |
38954-02-8
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| PubChem CID |
10614148
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| Appearance |
White to off-white solid powder
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| LogP |
-0.3
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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 |
5
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| Heavy Atom Count |
21
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| Complexity |
306
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1=CC(=CC=C1CCO)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O
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| InChi Key |
OJDSCNUKKOKOQJ-RKQHYHRCSA-N
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| InChi Code |
InChI=1S/C14H20O7/c15-6-5-8-1-3-9(4-2-8)20-14-13(19)12(18)11(17)10(7-16)21-14/h1-4,10-19H,5-7H2/t10-,11-,12+,13-,14-/m1/s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-2-[4-(2-hydroxyethyl)phenoxy]-6-(hydroxymethyl)oxane-3,4,5-triol
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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 | 3.3300 mL | 16.6500 mL | 33.3000 mL | |
| 5 mM | 0.6660 mL | 3.3300 mL | 6.6600 mL | |
| 10 mM | 0.3330 mL | 1.6650 mL | 3.3300 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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