2. Immunology/Inflammation Apoptosis Others
  3. NOD-like Receptor (NLR) Caspase Insecticide
  4. Phaseoloidin

Phaseoloidin is an orally active multi-target inhibitor. Phaseoloidin inhibits the activation of the NLRP3 inflammasome and blocks the caspase-11-GSDMD pyroptosis axis. Phaseoloidin reduces the expression of collagen-degrading enzymes to maintain the integrity of cartilage matrix. Phaseoloidin activates the AMPK/mTOR pathway to enhance autophagic function. Phaseoloidin exerts adverse effects on the growth and development of Manduca sexta and Spodoptera littoralis larvae, inhibits larval growth, and thereby helps Nicotiana attenuata defend against lepidopteran herbivorous insects. Phaseoloidin is applicable to research related to acute gouty arthritis and pulmonary fibrosis.

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Phaseoloidin

Phaseoloidin Chemical Structure

CAS No. : 118555-82-1

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Based on 1 publication(s) in Google Scholar

Phaseoloidin Related Antibodies

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Description

Phaseoloidin is an orally active multi-target inhibitor. Phaseoloidin inhibits the activation of the NLRP3 inflammasome and blocks the caspase-11-GSDMD pyroptosis axis. Phaseoloidin reduces the expression of collagen-degrading enzymes to maintain the integrity of cartilage matrix. Phaseoloidin activates the AMPK/mTOR pathway to enhance autophagic function. Phaseoloidin exerts adverse effects on the growth and development of Manduca sexta and Spodoptera littoralis larvae, inhibits larval growth, and thereby helps Nicotiana attenuata defend against lepidopteran herbivorous insects. Phaseoloidin is applicable to research related to acute gouty arthritis and pulmonary fibrosis[1][2][3].

In Vitro

Phaseoloidin directly binds to core components of the NLRP3 inflammasome pathway, including NLRP3, caspase-1, IL-1β, and GSDMD, with binding affinity values ranging from -6.543 to -7.588 kcal/mol[1].
Phaseoloidin (6.25-200 μM; 24 h) is non-cytotoxic to mouse peritoneal macrophages at concentrations up to 200 μM following 24 h incubation[1].
Phaseoloidin (6.25-200 μM; 24 h) is non-cytotoxic to rat articular chondrocytes at concentrations up to 100 μM following 24 h incubation, with only mild cytotoxicity at 200 μM[1].
Phaseoloidin (25-100 μM; 1 h pre-incubation, followed by 22 h total incubation with LPS and sodium urate crystals) dose-dependently inhibits NLRP3 inflammasome activation and downstream inflammatory mediator release in LPS/sodium urate-stimulated mouse peritoneal macrophages, with maximal effects at 100 μM[1].
Phaseoloidin (10-100 μM; 48 h) activates the AMPK/mTOR pathway to promote autophagy in TGF-β1-induced primary mouse lung myofibroblasts[2].
Phaseoloidin (3-300 μM) does not reduce the viability of TGF-β1-induced primary mouse lung myofibroblasts[2].
Phaseoloidin (10-100 μM; 48 h) promotes autophagy-mediated collagen degradation in TGF-β1-induced primary mouse lung myofibroblasts via the AMPK pathway[2].
Phaseoloidin (10-100 μM; 48 h co-treatment with FasL) reverses FasL-induced apoptosis resistance in TGF-β1-induced primary mouse lung myofibroblasts via the AMPK pathway[2].
Phaseoloidin (10-100 μM; 48 h co-treatment with FasL) promotes autophagy-mediated degradation of PTPN13 to restore FasL-induced apoptosis sensitivity in TGF-β1-induced primary mouse lung myofibroblasts[2].

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

Phaseoloidin Related Antibodies

Cell Viability Assay[1]

Cell Line: Rat articular chondrocytes
Concentration: 6.25-200 μM
Incubation Time: 24 h
Result: Showed no significant cytotoxicity at concentrations ≤100 μM relative to untreated cells.
Caused a minor but significant reduction in viability at 200 μM relative to untreated cells.
In Vivo

Phaseoloidin (25-100 mg/kg; i.g.; single dose 1 hour pre-challenge) dose-dependently ameliorates sodium urate-induced acute gouty arthritis in mice by inhibiting NLRP3 inflammasome activation, caspase-11-GSDMD-mediated pyroptosis, NETosis, and cartilage matrix degradation[1].
Phaseoloidin (25-100 mg/kg; i.g.; single dose 1 hour pre-challenge) dose-dependently suppresses sodium urate-induced acute gout inflammation in mouse air pouches by inhibiting NLRP3 inflammasome activation, pyroptosis, and NETosis, with high-dose treatment normalizing lavage fluid IL-1β levels[1].
Phaseoloidin (1-25 mg/kg; i.p.; daily; days 14-28) exerts dose-dependent antifibrotic effects in bleomycin-induced pulmonary fibrosis in male C57/BL mice via AMPK-mediated autophagy activation, with the 25 mg/kg dose producing the strongest reduction in fibrosis markers, mortality, and myofibroblast apoptosis resistance[2].
Phaseoloidin (0.16 μg/mg of diet; oral; continuous feeding; 12 days) reduces Manduca sexta larval growth by 50%[3].
Phaseoloidin (0.16 μg/mg of diet; oral; continuous feeding; 8 days) reduces Spodoptera littoralis larval growth by 55%[3].

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

Animal Model: Kunming mice (male, 6-8 weeks old, acute gouty arthritis induced by sodium urate crystal paw injection)[1]
Dosage: 25-100 mg/kg
Administration: i.g.; single dose 1 hour pre-challenge
Result: Attenuated paw swelling dose-dependently at 1 hour post-sodium urate injection.
Reduced paw erythema and swelling.
Decreased immune cell infiltration in articular cavity and periarticular muscle tissues.
Downregulated expression of macrophage marker F4/80 dose-dependently.
Inhibited expression of NLRP3 inflammasome components (NLRP3, ASC, pro-caspase-1, cleaved caspase-1, pro-IL-1β, mature IL-1β, HMGB1, Cathepsin B) dose-dependently.
Reduced levels of caspase-11 pathway proteins (pro-caspase-11, cleaved caspase-11, GSDMD, GSDMD-N) dose-dependently.
Suppressed sodium urate-induced expression of NETosis-associated proteins (Cathepsin G, CitH3, PAD4, PR3, NE) dose-dependently.
Reduced SYTOX Green-labeled extracellular DNA release.
Downregulated sodium urate-induced expression of cartilage-degrading enzymes MMP-3 and MMP-13 dose-dependently.
Restored paw glycosaminoglycan content (toluidine blue staining intensity).
Reduced cartilage erosion.
Animal Model: Kunming mice (male, 6-8 weeks old, acute gout induced by sodium urate crystal subcutaneous air pouch injection)[1]
Dosage: 25-100 mg/kg
Administration: i.g.; single dose 1 hour pre-challenge
Result: Reduced inflammatory cell infiltration in air pouch subcutaneous tissue dose-dependently.
Inhibited NLRP3 inflammasome activation (downregulated HMGB1, Cathepsin B, NLRP3, ASC, pro-caspase-1, cleaved caspase-1, pro-IL-1β, mature IL-1β) dose-dependently.
Suppressed caspase-11-GSDMD pathway activity (downregulated pro-caspase-11, cleaved caspase-11, GSDMD, GSDMD-N) dose-dependently.
Reduced IL-1β levels in air pouch lavage fluid from ~1800 pg/mL (model group) to near-normal levels (~300 pg/mL) at 100 mg/kg.
Inhibited sodium urate-induced NETosis dose-dependently, reducing expression of Cathepsin G, CitH3, PAD4, PR3, and NE.
Decreased co-localization of MPO and SYTOX Green signals.
Animal Model: C57/BL (male)[2]
Dosage: 1 mg/kg; 5 mg/kg; 25 mg/kg
Administration: i.p.; daily; days 14-28
Result: Reduced alveolar wall thickening and extracellular matrix deposition .
Dose-dependently reduced mortality, partially reversed bleomycin-induced weight loss, and lowered lung hydroxyproline content relative to untreated fibrotic mice.
Decreased bleomycin-induced upregulation of Collagen I and α-SMA mRNA and protein levels.
Activated AMPK phosphorylation in lung tissue, increased autophagic activity, and promoted myofibroblast sensitivity to FasL-induced apoptosis by reducing PTPN13 protein abundance.
Completely reversed antifibrotic, survival-improving, autophagy-activating, and apoptosis-sensitizing effects when co-administered with AMPK inhibitor Compound C .
Molecular Weight

330.29

Formula

C14H18O9
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1=CC(O)=CC=C1O[C@H]2[C@@H]([C@H]([C@@H]([C@@H](CO)O2)O)O)O
Structure Classification
Initial Source
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 (302.76 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 3.0276 mL 15.1382 mL 30.2764 mL
5 mM 0.6055 mL 3.0276 mL 6.0553 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 (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.

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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: ≥ 2.5 mg/mL (7.57 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (7.57 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:

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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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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.92%

SDS (393 KB)

COA (251 KB) HNMR (164 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References

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 3.0276 mL 15.1382 mL 30.2764 mL 75.6911 mL
5 mM 0.6055 mL 3.0276 mL 6.0553 mL 15.1382 mL
10 mM 0.3028 mL 1.5138 mL 3.0276 mL 7.5691 mL
15 mM 0.2018 mL 1.0092 mL 2.0184 mL 5.0461 mL
20 mM 0.1514 mL 0.7569 mL 1.5138 mL 3.7846 mL
25 mM 0.1211 mL 0.6055 mL 1.2111 mL 3.0276 mL
30 mM 0.1009 mL 0.5046 mL 1.0092 mL 2.5230 mL
40 mM 0.0757 mL 0.3785 mL 0.7569 mL 1.8923 mL
50 mM 0.0606 mL 0.3028 mL 0.6055 mL 1.5138 mL
60 mM 0.0505 mL 0.2523 mL 0.5046 mL 1.2615 mL
80 mM 0.0378 mL 0.1892 mL 0.3785 mL 0.9461 mL
100 mM 0.0303 mL 0.1514 mL 0.3028 mL 0.7569 mL
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Phaseoloidin Related Classifications

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  • 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:

Phaseoloidin118555-82-1NOD-like Receptor (NLR)CaspaseInsecticidecaspase-11caspase-1myofibroblastsFasLManduca sextaAMPK/mTOR pathwaybleomycin-induced pulmonary fibrosis mouse modelsGSDMDNLRP3 inflammasomeIL-1βInhibitorinhibitorinhibit

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