| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary target is the HBV RNA transcription and protein expression machinery. Helioxanthin 8-1 suppresses HBV RNA production dose-dependently, unlike lamivudine which does not affect HBV RNA. It also inhibits HBV DNA replication of both wild-type and 3TC-resistant virus. The compound interferes with viral RNA transcription and protein synthesis, possibly through modulation of host transcription factors. It also shows anti-HIV activity.
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|---|---|
| ln Vitro |
Helioxanthin 8-1 exhibits potent anti-HBV activity with an EC50 of 0.03 µM in human hepatoma cell lines and little cytotoxicity. It suppresses both HBV RNA and protein expression in a dose-dependent manner. It also inhibits HIV replication with an EC50 of 2.7 µM. It shows activity against 3TC-resistant HBV strains. It inhibits duck hepatitis B virus replication in cell culture.
|
| ln Vivo |
In vivo, helioxanthin 8-1 has demonstrated anti-HBV activity in animal models. It reduces viral RNA and DNA levels in duck HBV-infected models. It suppresses HBV replication in human HBV transgenic mice. Typical doses range from 1-50 mg/kg administered orally or intraperitoneally. It has a unique mechanism of action that may complement existing nucleoside analogues.
|
| Enzyme Assay |
HBV RNA quantification assays use human hepatoma cell lines (HepG2.2.15 or HuH-7) transfected with HBV. Cells are treated with helioxanthin 8-1 (0.001-10 µM) for 48-72 h. HBV RNA is extracted and quantified by Northern blotting or qRT-PCR. HBV DNA is measured by Southern blotting or qPCR. Cytotoxicity is assessed by MTT assay.
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| Cell Assay |
Cell-based antiviral assays use HepG2.2.15 cells cultured in DMEM with serum. Cells are treated with helioxanthin 8-1 at varying concentrations for 3-6 days. HBV surface antigen (HBsAg) and e antigen (HBeAg) are measured by ELISA. HBV DNA in culture supernatant is quantified by qPCR. Intracellular HBV RNA and DNA are measured by Northern and Southern blotting.
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| Animal Protocol |
In vivo, helioxanthin 8-1 is tested in duck HBV-infected ducklings or HBV transgenic mice. A typical protocol involves oral or intraperitoneal administration (1-50 mg/kg) daily for 2-4 weeks. Serum HBV DNA is measured by qPCR. Liver HBV RNA and DNA are quantified. Liver histopathology is assessed by H&E staining.
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| References |
| Molecular Formula |
C20H12N2O6
|
|---|---|
| Molecular Weight |
376.319085121155
|
| Exact Mass |
376.069
|
| CAS # |
840529-13-7
|
| Related CAS # |
Helioxanthin;18920-47-3
|
| PubChem CID |
6320331
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Index of Refraction |
1.715
|
| LogP |
3.29
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
28
|
| Complexity |
673
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1OC2=C(O1)C=C(C=C2)C3=C4C(=CC5=C3C(=O)NNC5=O)C=CC6=C4OCO6
|
| InChi Key |
PXSPEYYAEFFUMN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H12N2O6/c23-19-11-5-9-2-4-13-18(28-8-26-13)16(9)15(17(11)20(24)22-21-19)10-1-3-12-14(6-10)27-7-25-12/h1-6H,7-8H2,(H,21,23)(H,22,24)
|
| Chemical Name |
11-(1,3-benzodioxol-5-yl)-8,9-dihydro-[1,3]benzodioxolo[7,6-g]phthalazine-7,10-dione
|
| 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 : ~10 mg/mL (~26.57 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (2.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 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 | 2.6573 mL | 13.2866 mL | 26.5731 mL | |
| 5 mM | 0.5315 mL | 2.6573 mL | 5.3146 mL | |
| 10 mM | 0.2657 mL | 1.3287 mL | 2.6573 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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