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.
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- Purity : 99.71%
- CAS No.: 851518-71-3
- 화학식: C12H11NO2
- 분자량:201.22
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Hydronidone
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Biological Activity
제품 설명
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.
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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.
- Fibrosis/Collagen Morphometry
- Collagen: Sirius Red Staining
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- Research Protocol for Inflammation-related Diseases
- Liver Histomorphometry
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 No. 851518-71-3
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Appearance Solid
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분자량 201.22
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
용액&용해도
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.
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: ≥ 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.
순도&문서
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- 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)
References
[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 |
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| 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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