Autophagy Anti-infection Metabolic Enzyme/Protease Cell Cycle/DNA Damage NF-κB Immunology/Inflammation Apoptosis MAPK/ERK Pathway Cytoskeleton Stem Cell/Wnt PI3K/Akt/mTOR Membrane Transporter/Ion Channel
Autophagy Apoptosis HBV HCV HSP Reactive Oxygen Species (ROS) Bcl-2 Family Glutathione S-transferase p38 MAPK NF-κB Microtubule/Tubulin ERK JNK TNF Receptor Interleukin Related CDK Cyclin G-associated Kinase (GAK) mTOR P-glycoprotein Ferroptosis
Bicyclol

Cat. No.: HY-B0766

Bicyclol

(Synonyms: SY801)

Customer Review

Based on 1 Customer Validation

Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma.

For research use only. We do not sell to patients.

Purity: 99.91%
CAS No.: 118159-48-1
Formula: C₁₉H₁₈O₉
Molecular Weight:390.34

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Bicyclol Chemical Structure

CAS No.: 118159-48-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All HSP Isoforms :

All Bcl-2 Family Isoforms :

All p38 MAPK Isoforms :

All NF-κB Isoforms :

All ERK Isoforms :

All JNK Isoforms :

All TNF Receptor Isoforms :

All Interleukin Related Isoforms :

All CDK Isoforms :

All mTOR Isoforms :

In Vitro

Bicyclol (0.1-1 mmol/L, 3 h) inhibits the release of ALT and AST, as well as the production of MDA, in CCl₄-induced hepatotoxic Wistar rat hepatocytes in a dose-dependent manner^[1].
Bicyclol (40 and 80 μM; 1 h) reduces palmitic acid (HY-N0830)-induced apoptosis in human hepatocyte HL-7702 cells and inhibits palmitic acid (HY-N0830)-induced activation of MAPKs and NF-κB in macrophages^[2].
Bicyclol (200 μM; 10 h) reduces the level of intracellular oxygen free radicals in HCV-infected Huh7.5 cells and inhibits the phosphorylation of p38, ERK, JNK, and NF-κB^[4].
Bicyclol (10 μM; 30 min) alleviates serrata-induced hepatocyte inactivation, destruction, and lipid peroxidation. Bicyclol (0-500 μM; 0-48 h) effectively inhibits the proliferation of HepG2 cells in a dose-dependent and time-dependent manner^[5].
Bicyclol (0-100 μM; 24 h) reverses vincristine sulfate (HY-N0488) resistance in VinRKB cells by 2.8, 7.3, and 20.7 times, respectively^[6].
Bicyclol (50 and 100 μM; 12-72 h) alters the intracellular drug concentrations in vincristine sulfate (HY-N0488)-resistant human epidermoid carcinoma VinRKB and doxorubicin (HY-15142A)-resistant human breast cancer AdrRMCF-7 cells, sensitizing the resistant cells to anticancer drugs^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

CCL4-induced intoxication of Wistar rat hepatocytes
Concentration:

10^-4-10^-3 mol/L
Incubation Time:

3 h
Result:

Improved rat liver cell viability and reduced cell surface damage such as microvilli aggregation and shedding.

Cell Proliferation Assay^[6]

Cell Line:

HepG2 cells
Concentration:

50, 100, 200 and 500 μM
Incubation Time:

24 and 48 h
Result:

Inhibited the phosphorylation of Akt and ERK, and downregulates the expression of cyclin D1, cyclin E2, CDK2, CDK4, p-Rb, and p-mTOR.

Apoptosis Analysis^[2]

Cell Line:

Palmitic acid induces human hepatocyte HL-7702 cells
Concentration:

40 and 80 μM
Incubation Time:

1 h
Result:

Inhibited the expression of IL-6 and TNF-α induced by PA.

Western Blot Analysis^[8]

Cell Line:

Vincristine-resistant human epidermoid carcinoma VinRKB and doxorubicin-resistant human breast cancer AdrRMCF-7
Concentration:

50 and 100 μM
Incubation Time:

24-72 h
Result:

Reduced the level of p-glycoprotein encoded by the MDR-1 gene in VinRKB and AdrRMCF-7 cells to the level of drug-sensitive cells. The increase of GSH content in virrkb and AdrRMCF-7 cells increased the GST activity of AdrRMCF-7 cells, and the overexpression of Bcl-2 protein.

In Vivo

Bicyclol (50, 100 and 200 mg/kg; p.o.; single dose) has a dose-dependent protective effect against liver damage induced by different drugs in mice^[1].
Bicyclol (50 and 150 mg/kg; p.o.; once a day for 3 days) has a significant protective effect against Acetaminophen (HY-66005) induced mitochondrial damage in mouse hepatocytes^[1].
Bicyclol (150 mg/kg; p.o.; once a day for 3 days) inhibits the expression of Fas/FasL mRNA and the release of TNF-α in mouse hepatocytes induced by ConA and plays an anti-apoptotic role in hepatocytes^[1].
Bicyclol (300 mg/kg; p.o.; once daily for 3 days) alleviates ConA- and Acetaminophen (HY-66005) induced liver damage in mice, reducing serum transaminases, liver necrosis, mitochondrial cytochrome C and apoptosis-inducing factor (AIF) release, and liver DNA fragmentation^[1].
Bicyclol (75 and 150 mg/kg; p.o.; 6 times per week except Sunday for 7 weeks) significantly improves liver damage and fibrosis in rats and mice induces by chronic CCl4 and Dimethylnitosamine hepatotoxicity^1].
Bicyclol (25 and 50 mg/kg; p.o.; once every other day for 4 weeks) alleviates hyperlipidemia and liver damage and inhibites inflammatory signaling pathways in HFD-induced NAFLD mice^[2].
Bicyclol (200 mg/kg; i.p.; 3 times a day for 2 days) inhibits iron-induced apoptosis in the liver of CCl4-induced ALI mice and exerts a hepatoprotective effect^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CCl4, D-Galactosamine, Acetaminophen-Induced Liver Injury in Mice ^[1]
Dosage:

50, 100 and 200 mg/kg
Administration:

Oral gavage (p.o.) Single dose administration
Result:

Reduced the elevated serum ALT and AST levels in a dose-dependent manner, and also ameliorated the liver lesions.

Animal Model:

Acetaminophen-Induced Liver Injury in Mice ^[1]
Dosage:

50 and 150 mg/kg
Administration:

Oral gavage (p.o.); Once a day for 3 days
Result:

Reduced mitochondrial ultrastructural damage, mitochondrial AST release, mitochondrial fluidity and mitochondrial swelling, and mitochondrial cytochrome C release.

Animal Model:

ConA and acetaminophen-Induced Liver Injury in Mice ^[1]
Dosage:

300 mg/kg
Administration:

Oral gavage (p.o.); Once a day for 3 days
Result:

Induced the expression of HSP70/27 mRNA and protein in mouse liver and activated heat shock factor-1 (HSF1) in mouse liver.

Animal Model:

HFD-induced liver inflammation in mice^[2]
Dosage:

25 and 50 mg/kg
Administration:

Oral gavage (p.o.); once every other day for the last four weeks of the 16-week HFD induction
Result:

Inhibited the expression levels of pro-inflammatory genes IL-6, TNF-α, IL-1β, COX-2, ICAM-1, VCAM-1, and MCP-1.

Animal Model:

CCl4-induced ALI mice^[6].
Dosage:

200 mg/kg
Administration:

Intraperitoneal injection (i.p.); 3 times a day for 2 days
Result:

Inhibited iron accumulation, excessive production of reactive oxygen species, enhanced lipid peroxidation, altered mitochondrial morphology, and decreased GPx4 and xCT protein levels in mouse liver.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 118159-48-1
Appearance Solid
Molecular Weight 390.34
Formula C₁₉H₁₈O₉
Color White to off-white
SMILES

O=C(C1=CC(OC)=C(OCO2)C2=C1C3=C4OCOC4=C(OC)C=C3CO)OC
Synonyms

SY801
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (256.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5619 mL

12.8093 mL

25.6187 mL

5 mM

0.5124 mL

2.5619 mL

5.1237 mL

10 mM

0.2562 mL

1.2809 mL

2.5619 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (6.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.40 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 0.5% CMC-Na/0.5% Tween-80 in Saline water

Solubility: 1 mg/mL (2.56 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 15% Cremophor EL 85% Saline

Solubility: 2 mg/mL (5.12 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (293 KB)
SDS (398 KB)
- English - EN (398 KB)
- Français - FR (398 KB)
- Deutsch - DE (398 KB)
- Norwegian - NO (398 KB)
- Español - ES (398 KB)
- Swedish - SV (398 KB)
- Italian - IT (398 KB)
- Korean - KR (398 KB)
- Portuguese - PT (398 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Walsh, S.W., Y. Wang, and A. Killian, AA-2414, an antioxidant and thromboxane receptor blocker, completely inhibits peroxide-induced vasoconstriction in the human placenta. J Pharmacol Exp Ther, 1999. 290(1): p. 220-6. [Content Brief]

[2]. Weixin Zhao, et al. "Bicyclol ameliorates nonalcoholic fatty liver disease in mice via inhibiting MAPKs and NF-κB signaling pathways." Biomedicine & Pharmacotherapy 141 (2021): 111874. [Content Brief]

[3]. Hui-Juan Dai, et al. "Induction of heat shock protein 27 by bicyclol attenuates d-galactosamine/lipopolysaccharide-induced liver injury." European Journal of Pharmacology 791 (2016): 482-490. [Content Brief]

[4]. Li Hu, et al. "Bicyclol attenuates liver inflammation induced by infection of hepatitis C virus via repressing ROS-mediated activation of MAPK/NF-κB signaling pathway." Frontiers in Pharmacology 9 (2018): 1438. [Content Brief]

[5]. Tianming Zhao, et al. "Regulating Nrf2-GPx4 axis by bicyclol can prevent ferroptosis in carbon tetrachloride-induced acute liver injury in mice." Cell death discovery 8.1 (2022): 380. [Content Brief]

[6]. Yu Wang, et al. "Bicyclol induces cell cycle arrest and autophagy in HepG2 human hepatocellular carcinoma cells through the PI3K/AKT and Ras/Raf/MEK/ERK pathways." BMC cancer 16 (2016): 1-15. [Content Brief]

[7]. Tianming Zhao, et al. "Therapeutic potential of bicyclol in liver diseases: lessons from a synthetic drug based on herbal derivative in traditional Chinese medicine." International Immunopharmacology 91 (2021): 107308. [Content Brief]

[8]. Bing Zhu, et al. "Chemosensitizing multiple drug resistance of human carcinoma by Bicyclol involves attenuated P-glycoprotein, GST-P and Bcl-2." Cancer biology & therapy 5.5 (2006): 536-543. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5619 mL	12.8093 mL	25.6187 mL	64.0467 mL
	5 mM	0.5124 mL	2.5619 mL	5.1237 mL	12.8093 mL
	10 mM	0.2562 mL	1.2809 mL	2.5619 mL	6.4047 mL
	15 mM	0.1708 mL	0.8540 mL	1.7079 mL	4.2698 mL
	20 mM	0.1281 mL	0.6405 mL	1.2809 mL	3.2023 mL
	25 mM	0.1025 mL	0.5124 mL	1.0247 mL	2.5619 mL
	30 mM	0.0854 mL	0.4270 mL	0.8540 mL	2.1349 mL
	40 mM	0.0640 mL	0.3202 mL	0.6405 mL	1.6012 mL
	50 mM	0.0512 mL	0.2562 mL	0.5124 mL	1.2809 mL
	60 mM	0.0427 mL	0.2135 mL	0.4270 mL	1.0674 mL
	80 mM	0.0320 mL	0.1601 mL	0.3202 mL	0.8006 mL
	100 mM	0.0256 mL	0.1281 mL	0.2562 mL	0.6405 mL

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Bicyclol

Anti-Infection Compound Library

Apoptosis Compound Library

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