Cat. No.: HY-N0899

Wilforine

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Wilforine is an orally active JAK-STAT pathway inhibitor with immunomodulatory effects and the ability to inhibit osteoclast fusion. Wilforine disrupts lipid raft integrity, reprograms cholesterol and glycosphingolipid metabolic pathways, regulates NF-κB and the complement system, and modulates the expression of various interleukins. Wilforine also inhibits the Wnt11/β-catenin signaling pathway and suppresses the proliferation of fibroblast-like synoviocytes. Wilforine can serve as a quality and pharmacokinetic marker for Tripterygium glycoside tablets, and can be applied to research on related diseases such as rheumatoid arthritis, inflammatory osteolysis, and SAPHO syndrome.

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Pureté: 99.47%
CAS No.: 11088-09-8
Formule: C₄₃H₄₉NO₁₈
Masse moléculaire:867.85

Stockage:

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

Wilforine Chemical Structure

CAS No.: 11088-09-8

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

Wnt11

Voir tous les produits spécifiques à Isoform JAK :

Voir tous les produits spécifiques à Isoform STAT :

Voir tous les produits spécifiques à Isoform Wnt :

In Vitro

Wilforine (100 μM; 6 days) inhibits osteoclast fusion in RAW264.7 cells by suppressing the JAK-STAT pathway, reducing expression of lipid raft scaffold proteins Stomatin and Flotillin-1, disrupting lipid raft integrity, and impairing localization and expression of fusion-related proteins CD9 and DC-STAMP^[1].
Wilforine (200-400 nM) dose-dependently inhibits the proliferation of collagen-induced arthritis fibroblast-like synoviocytes (CIA FLS)^[2].
Wilforine (30-300 μM; 20 h) induces significant cytotoxicity in human hepatoma HepG2 cells at concentrations of 30, 100, and 300 μM, with viability decreasing in a concentration-dependent manner^[3].

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

Cell Proliferation Assay^[2]

Cell Line:

Wnt11-overexpressing collagen-induced arthritis fibroblast-like synoviocytes (CIA FLS)
Concentration:

400 nM (wilforine treatment); optimal MOI (adenovirus infection)
Incubation Time:

36-48 h (adenovirus infection before wilforine treatment)
Result:

Reduced relative CCK-8 detection value of CIA FLS from ~3.2 (untreated) to ~1.8 (wilforine-treated).
Reversed the inhibitory effect in Wnt11-overexpressing CIA FLS, with relative CCK-8 detection value increased to ~2.8.

Cell Cytotoxicity Assay^[3]

Cell Line:

human hepatoma HepG2 cells
Concentration:

30 μM; 100 μM; 300 μM
Incubation Time:

20 h
Result:

Caused a significant reduction in HepG2 relative viability compared to the control group at 30 μM.
Caused highly significant reductions in HepG2 relative viability compared to the control group at 100 μM and 300 μM.

In Vivo

Wilforine (10-20 mg/kg; p.o.; daily; 28 days) dose-dependently alleviates inflammatory osteolysis in Pstpip2^cmo mice^[1].
Wilforine (40-56 μg/kg; p.o.; daily; from day 7 post-first immunization through day 35 post-first immunization) dose-dependently alleviates collagen-induced arthritis in rats, with significant reductions in arthritis scores, inflammatory cytokines, and pathological gene expression via inhibition of the Wnt11/β-catenin signaling pathway^[2].
Wilforine (10-90 mg/kg; p.o.; daily; 21 days), administered as part of TGT suspension, dose-dependently reduces paw swelling in adjuvant arthritis rats and exhibits dose-dependent and time-dependent plasma AUC_0-tn values, with significant toxicity (4 deaths) observed at the 90 mg/kg dose^[3].

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

Animal Model:

C57BL/6N Pstpip2cmo mice (both male and female, 6 weeks old, body weight 25 g)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

p.o.; daily; 28 days
Result:

Significantly reduced arthritis scores and paw thickness compared to the model group, with the 20 mg/kg dose showing superior efficacy.
Reduced bone destruction and clearer joint margins in treated mice, with the 20 mg/kg dose showing greater improvement.
Demonstrated dose-dependent reductions in cartilage erosion, synovial hyperplasia, inflammatory cell infiltration, cartilage matrix degradation, and periarticular fibrosis; the 20 mg/kg dose restored near-normal cartilage structure and tidemark clarity.
Significantly suppressed joint and paw expression of pro-inflammatory cytokines IL-1β and IL-6, and increased anti-inflammatory cytokine IL-10 expression compared to the model group (20 mg/kg dose).
Significantly downregulated joint expression of lipid raft scaffold proteins Stomatin and Flotillin-1, and osteoclast fusion-related proteins CD9 and DC-STAMPcompared to the model group (20 mg/kg dose).

Animal Model:

Sprague-Dawley (SD) (male, 160-180 g, SPF grade, collagen-induced arthritis model)^[2]
Dosage:

40 μg/kg; 48 μg/kg; 56 μg/kg
Administration:

p.o.; daily; from day 7 post-first immunization through day 35 post-first immunization
Result:

Dose-dependently reduced arthritis scores, hind paw swelling, and pain sensitivity (increased paw withdrawal threshold), and restored body weight.
Dose-dependently reduced serum levels of IL-1β, IL-6, and TNF-α.
Decreased mRNA levels of MMP3 and fibronectin in joint synovium.
Alleviated synovial hyperplasia, pannus formation, and bone/cartilage damage.
Dose-dependently reduced mRNA levels of Wnt11, CCND1, GSK-3β, and c-Myc in synovium.

Chemical Information

CAS No. 11088-09-8
Appearance Solid
Masse moléculaire 867.85
Formule C₄₃H₄₉NO₁₈
Color White to off-white
SMILES

CC(OCC(C1OC(C)=O)(C(C(OC(C2=CC=CC=C2)=O)C3OC(C4C)=O)OC(C)=O)C(OC(C)(COC(C5=CC=CN=C5CC4)=O)C6C1OC(C)=O)(C3(O)C)C6OC(C)=O)=O
Structure Classification
- Terpenoids
- Sesquiterpenes
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (57.61 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

1.1523 mL

5.7614 mL

11.5227 mL

5 mM

0.2305 mL

1.1523 mL

2.3045 mL

10 mM

0.1152 mL

0.5761 mL

1.1523 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, 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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 (2.88 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.88 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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (296 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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)
Instruction de manipulation (2659 KB)

Références

[1]. Geng S, et al. Wilforine attenuates inflammatory osteolysis by suppressing osteoclast fusion through JAK-STAT-stomatin immunoregulatory signaling. Front Immunol. 2026;17:1789493. Published 2026 Mar 13. [Content Brief]

[2]. Huang Y, et al. Wilforine inhibits rheumatoid arthritis pathology through the Wnt11/β-catenin signaling pathway axis. Arthritis Res Ther. 2023;25(1):243. Published 2023 Dec 14. [Content Brief]

[3]. Gao X, et al. Wilforine, the Q-marker and PK-maker of Tripterygium glycosides tablet: Based on preparation quantitative analysis and PK-PD study. Phytomedicine. 2019;54:357-364. [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, 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	1.1523 mL	5.7614 mL	11.5227 mL	28.8068 mL
	5 mM	0.2305 mL	1.1523 mL	2.3045 mL	5.7614 mL
	10 mM	0.1152 mL	0.5761 mL	1.1523 mL	2.8807 mL
	15 mM	0.0768 mL	0.3841 mL	0.7682 mL	1.9205 mL
	20 mM	0.0576 mL	0.2881 mL	0.5761 mL	1.4403 mL
	25 mM	0.0461 mL	0.2305 mL	0.4609 mL	1.1523 mL
	30 mM	0.0384 mL	0.1920 mL	0.3841 mL	0.9602 mL
	40 mM	0.0288 mL	0.1440 mL	0.2881 mL	0.7202 mL
	50 mM	0.0230 mL	0.1152 mL	0.2305 mL	0.5761 mL

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Wilforine

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Natural Product Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Medicine Food Homology Compound Library

Terpenoids Library

Cytoskeleton Compound Library

Orally Active Compound Library

Traditional Chinese Medicine Active Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Cancer Natural Product Library

Anti-inflammatory Traditional Chinese Medicine Active Compound Library

Plant-Sourced Natural Product Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Antihypertensive Compound Library

Autoimmune Disease Compound Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Natural Product Library Plus

Natural Product and Natural Product-Like Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Miao Ethnicity Medicine Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

High-Throughput Natural Product Library

Ancient Chinese Classical Formulas Traditional Chinese Medicine Active Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Diarrhea-Related Traditional Chinese Medicine Active Compound Library

Mongolian Medicine Compound Library

Natural Product Diversity Scaffold Library

Mass Spectrometry Natural Product Library

Voir tous les produits spécifiques à Isoform JAK

Voir tous les produits spécifiques à Isoform STAT

Voir tous les produits spécifiques à Isoform Wnt

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Wilforine Related Classifications

HY-N0899 Related Classifications