2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation Stem Cell/Wnt TGF-beta/Smad
  3. Apoptosis Mitochondrial Metabolism Phosphodiesterase (PDE) COX TGF-beta/Smad
  4. Hydronidone

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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Hydronidone Chemical Structure

Hydronidone Chemical Structure

CAS No. : 851518-71-3

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Based on 1 publication(s) in Google Scholar

Hydronidone Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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COX COX-1 COX-2 COX-3

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Description

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[1][2][3].

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.

Hydronidone Related Antibodies

Apoptosis Analysis[2]

Cell Line: LX-2 cells
Concentration: 400 μM
Incubation Time: 24 h
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.

Western Blot Analysis[2]

Cell Line: LX-2 cells (hepatic stellate cells)
Concentration: 400 μM
Incubation Time: 24 h
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 (50-100 mg/kg; p.o.) ameliorates CCl4-induced and DDC-induced liver fibrosis and hepatic injury in mice[1].
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.

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]
Dosage: 50, 100 mg/kg
Administration: Oral gavage (p.o.)
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
Molecular Weight

201.22

Formula

C12H11NO2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C=CC(C)=CN1C2=CC=C(O)C=C2
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 (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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.9697 mL 24.8484 mL 49.6968 mL
5 mM 0.9939 mL 4.9697 mL 9.9394 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 Dissolution Calculator
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Purity & Documentation

Purity: 99.92%

SDS (392 KB)

COA (248 KB) HNMR (227 KB) LCMS (255 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 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
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Hydronidone 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:

Hydronidone851518-71-3ApoptosisMitochondrial MetabolismPhosphodiesterase (PDE)COXTGF-beta/SmadCyclooxygenaseTransforming growth factor betaantifibroticagenthepatic fibrosispyridine derivativeanti-inflammationanti-cancermitochondrialInhibitorinhibitorinhibit

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