Hydronidone
Based on 1 publication(s) in Google Scholar
Hydronidone is an orally active pyridine derivative. Hydronidone is an inhibitor of phosphodiesterase-4 (PDE4) and cyclo-oxygenase (COX) as well as TGF-β. Hydronidone induces mitochondrial dysfunction and triggers apoptosis. Hydronidone can be used for liver fibrosis, anti-inflammation and anti-cancer study.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.71%
- CAS. Nr.: 851518-71-3
- Formel: C12H11NO2
- Molecular Weight:201.22
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Hydronidone
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Biologische Aktivität
Beschreibung
In Vitro
Hydronidone (200-400 μM) inhibits the activation of hepatic stellate cells (HSCs) and inhibits liver fibrosis through regulation of Smad7 expression[1].
Hydronidone (400 μM) promotes TGFβRI degradation through Smad7 in a ubiquitin-proteasome-dependent pathway in HSCs[1].
Hydronidone (400 μM, 24 h) significantly promotes apoptosis in activated hepatic stellate cells (aHSCs) through mitochondrial (intrinsic) pathway in LX-2 cells[2].
Hydronidone (400 μM, 24 h) triggers endoplasmic reticulum stress (ERS) and subsequently activated the IRE1α-ASK1-JNK pathway[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:LX-2 cells
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Concentration:400 μM
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Incubation Time:24 h
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Result:Increased the number of apoptotic cells co-treated with TGF-β1.
Reversed the effect of TGF-β1 treatment which induced activation of HSCs as evidenced by increased expression of α-SMA and COL1A1 at both the protein and RNA levels.
Decreased the expression of Bcl-2 and increased the expression of Bax at both the protein and mRNA levels.
Significantly promoted the flow of cytochrome c from the mitochondria to the cytoplasm, indicating impairment of mitochondrial outer membrane permeabilization (MOMP).
Upregulated cleaved-caspase-3/full-length caspase-3 ratio.
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Cell Line:LX-2 cells (hepatic stellate cells)
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Concentration:400 μM
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Incubation Time:24 h
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Result:Reversed the effect of TGF-β1-induced activation of HSCs as evidenced by increased expression of α-SMA and COL1A1 at both the protein and RNA levels.
Decreased the expression of Bcl-2 and increased the expression of Bax at both the protein and mRNA levels.
Expression of Bip was significantly upregulated at both the protein and mRNA levels.
Increased the phosphorylated IRE1α (p-IRE1α) level.
Upregulated the level of p-ASK1 and p-JNK, two downstream factors of p-IRE1α.
In Vivo
Hydronidone significantly promotes apoptosis in activated hepatic stellate cells (aHSCs) in the CCl4- and DDC-induced liver fibrosis in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five-week-old male C57BL/6J mice (intraperitoneally injected with 10% carbon tetrachloride (CCl4) in corn oil at 5 μL/g of body weight, three times per week, for 6 weeks; or fed a diet containing 1% 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC) for 4 weeks)[1]
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Dosage:50, 100 mg/kg
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Administration:Oral gavage (p.o.)
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Result:The levels of hepatic inflammatory infiltration were improved.
Significantly reduced the collagen fibre content.
Decreased the hepatic hydroxyproline content.
Significantly reduced the mRNA levels of fibrosis-related genes, including Acta2, Col1a1, Col3a1, Mmp9 and Timp1.
Reduced the levels of α-SMA and collagen 1 (Col1) in liver tissues.
Upregulated Smad7 protein expression.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 851518-71-3
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Appearance Solid
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Molecular Weight 201.22
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Formel C12H11NO2
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Color Off-white to light yellow
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SMILES
O=C1C=CC(C)=CN1C2=CC=C(O)C=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Pharmacol Transl Sci
Hydronidone Mitigates Pulmonary Fibrosis by Regulating the TGF-β/Smad2/3 Axis in in Vitro and in Vivo Models. [Abstract]2025 Oct 6;8(11):3984-4000. PMID: 41262559
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (496.97 mM; ultrasonic and warming and heat to 60°C; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 1.25 mg/mL (6.21 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (49.70 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Protokoll
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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
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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.
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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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
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Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Liver Histomorphometry
Liver histomorphometry is a quantitative histological approach used to measure structural alterations in hepatic tissue, including parenchymal loss, steatosis, fibrosis, and vascular remodeling, by combining stained tissue section analysis with stereological or computerized image-based measurements. Classical morphometric frameworks quantify volume fractions of liver compartments and fibrotic regions using systematic sampling and image analysis, enabling objective comparison of pathological changes across experimental groups. These approaches are widely applied in liver cirrhosis and fibrosis studies to reduce subjectivity in histological scoring and improve reproducibility of tissue evaluation. Recent methodological advances integrate automated image analysis and radiomics-based extraction of histological features from standard liver stains (e. g. , H&E and fibrotic stains), enabling quantitative correlation between morphometric features and fibrosis stages in non-alcoholic fatty live
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (393 KB)
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- Français - FR (393 KB)
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- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Xu X, et al. Hydronidone ameliorates liver fibrosis by inhibiting activation of hepatic stellate cells via Smad7-mediated degradation of TGFβRI. Liver Int. 2023 Nov;43(11):2523-2537. [Content Brief]
[2]. Sun Z, et al. Hydronidone induces apoptosis in activated hepatic stellate cells through endoplasmic reticulum stress-associated mitochondrial apoptotic pathway. J Gastroenterol Hepatol. 2024 Aug;39(8):1695-1703. [Content Brief]
[3]. Juillerat-Jeanneret L, et al. Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. J Med Chem. 2018 Nov 21;61(22):9811-9840. [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 | 4.9697 mL | 24.8484 mL | 49.6968 mL | 124.2421 mL |
| 5 mM | 0.9939 mL | 4.9697 mL | 9.9394 mL | 24.8484 mL | |
| 10 mM | 0.4970 mL | 2.4848 mL | 4.9697 mL | 12.4242 mL | |
| 15 mM | 0.3313 mL | 1.6566 mL | 3.3131 mL | 8.2828 mL | |
| 20 mM | 0.2485 mL | 1.2424 mL | 2.4848 mL | 6.2121 mL | |
| 25 mM | 0.1988 mL | 0.9939 mL | 1.9879 mL | 4.9697 mL | |
| 30 mM | 0.1657 mL | 0.8283 mL | 1.6566 mL | 4.1414 mL | |
| 40 mM | 0.1242 mL | 0.6212 mL | 1.2424 mL | 3.1061 mL | |
| 50 mM | 0.0994 mL | 0.4970 mL | 0.9939 mL | 2.4848 mL | |
| 60 mM | 0.0828 mL | 0.4141 mL | 0.8283 mL | 2.0707 mL | |
| 80 mM | 0.0621 mL | 0.3106 mL | 0.6212 mL | 1.5530 mL | |
| 100 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2424 mL |
Hydronidone Related Classifications
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