Helioxanthin 8-1 (Synonyms: Helioxanthin analogue 8-1)

Cat. No.: HY-16680 Purity: 98.0%: Data Sheet
COA

SDS
Handling Instructions
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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.

Helioxanthin 8-1 Chemical Structure

CAS No. : 840529-13-7

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Other Forms of Helioxanthin 8-1:

Helioxanthin In-stock

2 Publications Citing Use of MCE Helioxanthin 8-1

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	CC₅₀	29 μM Compound: 8-1	Cytotoxicity against HBV transfected human HepG2 cells by MTT assay Cytotoxicity against HBV transfected human HepG2 cells by MTT assay	[PMID: 17488817]
HepG2	IC₅₀	> 1 μM Compound: 8-1	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	[PMID: 17488817]
HepG2 2.2.15	CC₅₀	9 μM Compound: 5	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]
HepG2 2.2.15	CC₅₀	9 μM Compound: 8-1	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	[PMID: 17488817]
HepG2 2.2.15	IC₅₀	0.08 μM Compound: 8-1	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	[PMID: 17488817]
HepG2 2.2.15	IC₅₀	0.3 μM Compound: 8-1	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	[PMID: 17488817]
HepG2 2.2.15	IC₅₀	0.9 μM Compound: 8-1	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	[PMID: 17488817]

In Vitro

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.

Cell Cytotoxicity Assay^[1]

Cell Line:	doxycycline-induced (viral replication active) and non-induced (no viral replication) dstet5 cells
Concentration:	10, 30, 50 μM
Incubation Time:	3 days (after 3 days of induction or non-induction)
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.

Cell Cytotoxicity Assay^[2]

Cell Line:	Vero cells (ATCC CCL-81)
Concentration:	100 μM
Incubation Time:	48 h
Result:	Reduced Vero cell viability to 70.6%. Exhibited a CC₅₀ value of >100 μM.

Molecular Weight

376.32

Formula

C₂₀H₁₂N₂O₆

CAS No.

840529-13-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NNC(C2=C(C3=CC=C(OCO4)C4=C3)C5=C6C(OCO6)=CC=C5C=C21)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 98.58%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (260 KB) HNMR (130 KB) RP-HPLC (164 KB)

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

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

Helioxanthin 8-1 Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Helioxanthin 8-1840529-13-7Helioxanthin analogue 8-1HBVHepatitis B virusanti-HBV agentdstet5 cellsVero cellsInhibitorinhibitorinhibit

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