| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Sempervirine nitrate targets the Wnt/beta-catenin signaling pathway and also acts as a specific molecular inhibitor of Mdm2. It inhibits the Wnt/beta-catenin pathway, suppressing HCC proliferation and inducing apoptosis. By targeting Mdm2, it abrogates Period 2 ubiquitination in MEF cells, leading to accumulation of a stable pool of Period 2.
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|---|---|
| ln Vitro |
In vitro, Sempervirine nitrate inhibits the proliferation of hepatocellular carcinoma (HCC) cells and induces apoptosis through regulation of the Wnt/beta-catenin pathway. It demonstrates significant anti-proliferative effects on HCC cells, promoting apoptosis and inhibiting cell growth in a concentration-dependent manner.
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| ln Vivo |
In vivo, Sempervirine nitrate inhibits HCC tumor growth and enhances the antitumor effects of sorafenib in animal models. It has been shown to effectively reduce tumor burden and improve the efficacy of standard chemotherapeutic agents, making it a promising candidate for combination therapy research in hepatocellular carcinoma.
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| Enzyme Assay |
Cells (e.g., MEFs or HCC lines) are lysed and incubated with varying concentrations of Sempervirine nitrate for 30 min at 4degC. The Mdm2 inhibitor abrogates Period 2 ubiquitination, assessed via immunoprecipitation of Period 2 followed by ubiquitin Western blot. Alternatively, purified Mdm2 and ubiquitination components are used.
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| Cell Assay |
Hepatocellular carcinoma cells (e.g., HepG2, Huh7) are seeded in 96-well plates and treated with Sempervirine nitrate at various concentrations for 24-72 hours. Cell viability is assessed using MTT or CCK-8 assays, and apoptosis is measured via flow cytometry using Annexin V/PI staining.
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| Animal Protocol |
Animal studies are conducted in nude mice bearing subcutaneous HCC xenografts. Mice receive Sempervirine nitrate via oral gavage or intraperitoneal injection, alone or in combination with sorafenib. Tumor volumes are measured bi-weekly with calipers. Tumor growth inhibition (TGI) is calculated, and tumor tissues are collected for Western blot analysis of Wnt/beta-catenin pathway proteins.
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| ADME/Pharmacokinetics |
The pharmacokinetic (PK) profile of Sempervirine nitrate supports its use as an in vivo research tool. Studies demonstrate that it possesses favorable properties for systemic administration, achieving sufficient exposure to modulate the Wnt/beta-catenin pathway and inhibit tumor growth in xenograft models.
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| Toxicity/Toxicokinetics |
Sempervirine nitrate has been evaluated in preclinical models and shows a favorable safety profile at therapeutic doses. As a natural alkaloid, it is generally well-tolerated in animal studies, with no significant off-target toxicities reported at effective concentrations. It is a research-grade compound not intended for human consumption.
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| References | |
| Additional Infomation |
Sempervirine nitrate is a pure compound, is well-defined, and is intended for research use only. It is a promising lead for the development of novel anticancer agents targeting the Wnt/beta-catenin pathway and Mdm2-mediated ubiquitination. However, it has not received regulatory approval for clinical use.
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| Molecular Formula |
C19H17N3O3
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|---|---|
| Molecular Weight |
335.36
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| Exact Mass |
337.143
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| CAS # |
17994-15-9
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| Related CAS # |
Sempervirine;549-92-8
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| PubChem CID |
167688
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.482
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
25
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| Complexity |
414
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC2=CC3=C4NC5C=CC=CC=5C4=CC=N3C=C2CC1.ON(O)=O
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| InChi Key |
NPMOCMWCFIQGMK-UHFFFAOYSA-O
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| InChi Code |
InChI=1S/C19H16N2.NO3/c1-2-6-14-12-21-10-9-16-15-7-3-4-8-17(15)20-19(16)18(21)11-13(14)5-1;2-1(3)4/h3-4,7-12H,1-2,5-6H2;/q;-1/p+1
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| Chemical Name |
16,17,18,19-tetrahydro-3H-yohimban-13-ium;nitrate
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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 |
| 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 | 2.9819 mL | 14.9094 mL | 29.8187 mL | |
| 5 mM | 0.5964 mL | 2.9819 mL | 5.9637 mL | |
| 10 mM | 0.2982 mL | 1.4909 mL | 2.9819 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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