Helioxanthin 8-1
Based on 2 publication(s) in Google Scholar
Helioxanthin 8-1(Helioxanthin analogue 8-1) is an anti-HBV agent. Helioxanthin 8-1 exhibits anti-hepatitis B virus activity in both in vitro human hepatitis B virus models and animal models. Helioxanthin 8-1 inhibits the synthesis of duck hepatitis B virus (DHBV) DNA, covalently closed circular DNA, RNA and proteins, thereby blocking DHBV replication. Helioxanthin 8-1 shows higher cytotoxicity in virus-induced cells than in non-induced cells. Helioxanthin 8-1 can be used in studies related to hepatitis B virus infection.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 840529-13-7
- Formula: C20H12N2O6
- Molecular Weight:376.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Helioxanthin 8-1
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | CC50 |
29 μM
Compound: 45505
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Cytotoxicity against HBV transfected human HepG2 cells by MTT assay
Cytotoxicity against HBV transfected human HepG2 cells by MTT assay
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[PMID: 17488817] |
| HepG2 | IC50 |
>1 μM
Compound: 45505
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Inhibition of HBV promoter in human HepG2 cells by luciferase reporter gene assay
Inhibition of HBV promoter in human HepG2 cells by luciferase reporter gene assay
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[PMID: 17488817] |
| HepG2 2.2.15 | IC50 |
0.08 μM
Compound: 8-1
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Antiviral activity against HBV in ayw wild type HepG2(2.2.15) cells assessed as inhibition of viral DNA replication
Antiviral activity against HBV in ayw wild type HepG2(2.2.15) cells assessed as inhibition of viral DNA replication
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[PMID: 17488817] |
| HepG2 2.2.15 | IC50 |
0.3 μM
Compound: 8-1
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Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as inhibition of viral pre-genomic RNA replication
Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as inhibition of viral pre-genomic RNA replication
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[PMID: 17488817] |
| HepG2 2.2.15 | IC50 |
0.9 μM
Compound: 8-1
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Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as inhibition of viral 2.4/2.1RNA replication
Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as inhibition of viral 2.4/2.1RNA replication
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[PMID: 17488817] |
| HepG2 2.2.15 | CC50 |
9 μM
Compound: 45505
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Cytotoxicity against HBV transfected human ayw wild type HepG2(2.2.15) cells by MTT assay
Cytotoxicity against HBV transfected human ayw wild type HepG2(2.2.15) cells by MTT assay
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[PMID: 17488817] |
| HepG2 2.2.15 | CC50 |
9 μM
Compound: 5
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Cytotoxicity against human HepG2(2.2.15) cells assessed as reduction in cell viability after 3 days by methylene blue assay
Cytotoxicity against human HepG2(2.2.15) cells assessed as reduction in cell viability after 3 days by methylene blue assay
|
[PMID: 28383274] |
Helioxanthin 8-1 (0.1-3 μM; 6 days) potently inhibits DHBV replication in induced dstet5 cells, with an IC50 value of 0.25 μM against viral DNA, 0.1 μM against viral RNA, and 0.1 μM against core protein. It also reduces cccDNA levels in a dose-dependent manner[1].
Helioxanthin 8-1 (0.03-0.3 μM; 6 days, in combination with 3TC) exhibits additive anti-DHBV activity in dstet5 cells when used in combination with 3TC (HY-B0250). Enhanced viral DNA inhibition is observed across the combined concentration range, with a CI value of 0.82[1].
Helioxanthin 8-1 (10-50 μM; 3 days) exhibits higher cytotoxicity towards virus-induced dstet5 cells (CC50 = 18 μM) than towards uninduced dstet5 cells (CC50 = 45 μM)[1].
Helioxanthin 8-1 (100 μM; 48 h) reduces the viability of Vero cells (ATCC CCL-81) to 70.6%, with a CC50 value of >100 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:doxycycline-induced (viral replication active) and non-induced (no viral replication) dstet5 cells
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Concentration:10, 30, 50 μM
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Incubation Time:3 days (after 3 days of induction or non-induction)
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Result:Had a mean ± sd CC50 of 18 μM in viral-induced dstet5 cells.
Had a mean ± sd CC50 of 45 μM in non-induced dstet5 cells.
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Cell Line:Vero cells (ATCC CCL-81)
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Concentration:100 μM
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Incubation Time:48 h
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Result:Reduced Vero cell viability to 70.6%.
Exhibited a CC50 value of >100 μM.
Chemical Information
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CAS No. 840529-13-7
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Appearance Solid
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Molecular Weight 376.32
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Formula C20H12N2O6
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Color Light yellow to yellow
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SMILES
O=C1NNC(C2=C(C3=CC=C(OCO4)C4=C3)C5=C6C(OCO6)=CC=C5C=C21)=O
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Synonyms
Helioxanthin analogue 8-1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Microorganisms
2021 Feb 25;9(3):471. PMID: 33668694 -
ACS Infect Dis
Discovery of New Hepatitis B Virus Capsid Assembly Modulators by an Optimal High-Throughput Cell-Based Assay. [Abstract]2019 May 10;5(5):778-787. PMID: 30761887
Solvent & Solubility
DMSO : 10 mg/mL (26.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.66 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.66 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Ying C, et al. Helioxanthin analogue 8-1 inhibits duck hepatitis B virus replication in cell culture. Antivir Chem Chemother. 2010;21(2):97-103. [Content Brief]
[2]. Stefanik M, et al. Antiviral Activity of Vacuolar ATPase Blocker Diphyllin against SARS-CoV-2. Microorganisms. 2021;9(3):471. Published 2021 Feb 25. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6573 mL | 13.2866 mL | 26.5731 mL | 66.4328 mL |
| 5 mM | 0.5315 mL | 2.6573 mL | 5.3146 mL | 13.2866 mL | |
| 10 mM | 0.2657 mL | 1.3287 mL | 2.6573 mL | 6.6433 mL | |
| 15 mM | 0.1772 mL | 0.8858 mL | 1.7715 mL | 4.4289 mL | |
| 20 mM | 0.1329 mL | 0.6643 mL | 1.3287 mL | 3.3216 mL | |
| 25 mM | 0.1063 mL | 0.5315 mL | 1.0629 mL | 2.6573 mL |