Mogroside III-E
Based on 1 Customer Validation
Mogroside III-E is a cucurbitane-type triterpenoid glycoside extracted from Siraitia grosvenorii, and it is an orally active TLR4 inhibitor. Mogroside III-E downregulates the expression of TLR4 and MyD88, and blocks the phosphorylation of downstream ERK, JNK and p38 MAPK molecules; meanwhile, it inhibits TGF-β- or LPS-mediated transdifferentiation of primary pulmonary fibroblasts into myofibroblasts, reduces the content of fibrosis markers such as hydroxyproline, suppresses the pro-fibrotic TGF-β/Smad signaling pathway, and downregulates the levels of inflammatory factors MPO and IL-1β. Mogroside III-E alleviates Bleomycin (HY-108345)-induced pulmonary collagen deposition and inflammatory infiltration in mice. Mogroside III-E can be used in studies related to idiopathic pulmonary fibrosis.
For research use only. We do not sell to patients.
- Purity : 99.30%
- CAS No.: 88901-37-5
- Formula: C48H82O19
- Molecular Weight:963.15
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
Description
IC50 & Target
[2]|
TLR4 |
ERK |
JNK |
p38 MAPK |
IL-1β |
In Vitro
Mogroside III-E (1% (w/v); 4-7 days) is produced by Saccharomyces cerevisiae las21Δ mutant which completely converts mogroside V to mogroside III-E, resulting in 100% relative abundance of mogroside III-E after 7 days of fermentation[1].
Mogroside III-E (MGIIIE) (3.125-50 μM; 24 h) potently inhibits LPS-induced NO release in RAW264.7 cells with an IC50 of 10.22 μM, exhibiting stronger anti-inflammatory activity than other tested mogrosides[2].
Mogroside III-E (10 μM; 48 h) inhibits TGF-β1-induced fibroblast activation, extracellular matrix deposition, and TLR4/MyD88-MAPK signaling in primary mouse lung fibroblasts, with no observed cytotoxicity at concentrations up to 100 μM[2].
Mogroside III-E (10 μM; 48 h) inhibits LPS-induced fibroblast activation and collagen production in primary mouse lung fibroblasts, likely acting primarily through the TLR4 signaling pathway[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:LPS-activated RAW264.7 cells
-
Concentration:12.5, 25, 50, 100 μM
-
Incubation Time:24 h
-
Result:Showed no cytotoxicity at concentrations ranging from 12.5 to 100 μM.
-
Cell Line:primary mouse lung fibroblasts (PLFs)
-
Concentration:0.1, 1, 10, 100 μM
-
Incubation Time:48 h
-
Result:Showed no cytotoxicity at concentrations ranging from 0.1 to 100 μM.
-
Cell Line:primary mouse lung fibroblasts (PLFs)
-
Concentration:10 μM
-
Incubation Time:48 h
-
Result:Significantly reduced TGF-β1-induced increases in α-SMA and collagen I protein expression, nearly restoring levels to those of untreated control cells.
Inhibited TGF-β1-induced upregulation of TLR4, MyD88, and phosphorylation of JNK, ERK, and p38 MAPKs.
-
Cell Line:primary mouse lung fibroblasts (PLFs)
-
Concentration:10 μM
-
Incubation Time:48 h; 1.5 h (TAK-242 pretreatment)
-
Result:Significantly reduced LPS-induced increases in α-SMA and collagen I protein expression.
Inhibited LPS-induced upregulation of TLR4.
Showed no additional reduction of α-SMA and collagen I levels when co-treated with TAK-242 compared to Mogroside III-E alone.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (male, 6-8 weeks old, 20 g)[2]
-
Dosage:1 mg/kg; 10 mg/kg; 20 mg/kg
-
Administration:p.o.; daily; 14 days
-
Result:Mitigated bleomycin-triggered weight loss and mortality in mice at 10 and 20 mg/kg, outperforming prednisone positive control.
Alleviated pulmonary edema, alveolar thickening and neutrophil infiltration across all dosages, with optimal anti-inflammatory and anti-fibrotic effects at 10 and 20 mg/kg.
Suppressed elevated lung MPO activity and IL-1β concentration at 10 and 20 mg/kg.
Decreased hydroxyproline, α-SMA, Col I and TIMP-1 levels, upregulated MMP-9, and normalized MMP-9/TIMP-1 balance at 10 and 20 mg/kg.
Blocked TGF-β/Smad2/3 cascade activation by lowering TGF-β1 and p-Smad2/3 expression at 10 and 20 mg/kg.
Repressed TLR4-MyD88 axis and downstream phosphorylated JNK, ERK and p38 MAPK signaling at 10 and 20 mg/kg.
Chemical Information
-
CAS No. 88901-37-5
-
Appearance Solid
-
Molecular Weight 963.15
-
Formula C48H82O19
-
Color White to off-white
-
SMILES
C[C@]12[C@](CC=C3[C@@]2([H])CC[C@H](O[C@]4([H])O[C@@H]([C@@H](O)[C@H](O)[C@H]4O)CO)C3(C)C)([H])[C@]5([C@@](C)([C@]([C@H](C)CC[C@H](C(C)(O)C)O[C@H]6[C@@H]([C@H]([C@H](O)[C@@H](CO)O6)O)O[C@]7([H])O[C@@H]([C@@H](O)[C@H](O)[C@H]7O)CO)([H])CC5)C[C@H]1O)C
-
Structure Classification
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (103.83 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 (protect from light). 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 (protect from light). 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.60 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.
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: ≥ 2.5 mg/mL (2.60 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 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:
-
-
-
-
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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Protocols
-
Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
-
Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
-
RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
-
Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
-
Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
-
Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
-
Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
-
Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
Purity & Documentation
-
Data Sheet (295 KB)
-
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)
-
Handling Instructions (2659 KB)
References
[1]. Wang R, et al. Dekkera bruxellensis, a beer yeast that specifically bioconverts mogroside extracts into the intense natural sweetener siamenoside I. Food chemistry. 2019 Mar 15;276:43-49. [Content Brief]
[2]. Tao L, et al. Mogroside IIIE, a Novel Anti-Fibrotic Compound, Reduces Pulmonary Fibrosis through Toll-Like Receptor 4 Pathways. Journal of Pharmacology and Experimental Therapeutics. 2017;361(2):268-279. [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 (protect from light). 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 | 1.0383 mL | 5.1913 mL | 10.3826 mL | 25.9565 mL |
| 5 mM | 0.2077 mL | 1.0383 mL | 2.0765 mL | 5.1913 mL | |
| 10 mM | 0.1038 mL | 0.5191 mL | 1.0383 mL | 2.5956 mL | |
| 15 mM | 0.0692 mL | 0.3461 mL | 0.6922 mL | 1.7304 mL | |
| 20 mM | 0.0519 mL | 0.2596 mL | 0.5191 mL | 1.2978 mL | |
| 25 mM | 0.0415 mL | 0.2077 mL | 0.4153 mL | 1.0383 mL | |
| 30 mM | 0.0346 mL | 0.1730 mL | 0.3461 mL | 0.8652 mL | |
| 40 mM | 0.0260 mL | 0.1298 mL | 0.2596 mL | 0.6489 mL | |
| 50 mM | 0.0208 mL | 0.1038 mL | 0.2077 mL | 0.5191 mL | |
| 60 mM | 0.0173 mL | 0.0865 mL | 0.1730 mL | 0.4326 mL | |
| 80 mM | 0.0130 mL | 0.0649 mL | 0.1298 mL | 0.3245 mL | |
| 100 mM | 0.0104 mL | 0.0519 mL | 0.1038 mL | 0.2596 mL |