| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Citiolone is a potent inhibitor of the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which is involved in the metabolism of cortisol. By inhibiting 11β-HSD1, citiolone may modulate glucocorticoid levels and reduce inflammation. It also acts as a potent antioxidant, reducing oxidative stress by scavenging free radicals. The compound supports liver function and promotes the regeneration of liver cells.
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|---|---|
| ln Vitro |
Citiolone acts as a potent antioxidant, reducing oxidative stress and inflammation in vitro. It supports liver function by protecting hepatocytes from damage and promoting regeneration. As an 11β-HSD1 inhibitor, it may modulate cortisol metabolism in cells. These activities contribute to its hepatoprotective and anti-inflammatory effects.
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| ln Vivo |
In vivo, citiolone has been studied for its hepatoprotective effects in liver disorders, including hepatitis and cirrhosis. It has been investigated in clinical trials up to Phase II. The compound reduces oxidative stress and inflammation in the liver, supporting liver function and promoting the regeneration of liver cells. Its mucolytic properties may also be beneficial for respiratory conditions.
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| Enzyme Assay |
In vitro assays for citiolone involve measuring its antioxidant activity and its inhibition of 11β-HSD1. Antioxidant activity is assessed using assays such as DPPH radical scavenging, ABTS, or FRAP. For 11β-HSD1 inhibition, recombinant enzyme or cell lysates are incubated with cortisol and NADPH in the presence of citiolone, and the conversion to cortisone is measured by HPLC or LC-MS/MS.
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| Cell Assay |
Cellular assays for citiolone are performed using hepatocyte cell lines (e.g., HepG2). Cells are treated with citiolone at varying concentrations, and oxidative stress is induced using agents such as H2O2 or CCl4. Cell viability, ROS production, and markers of oxidative stress (e.g., GSH, MDA) are measured. The compound's effects on inflammatory cytokine production may also be assessed.
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| Animal Protocol |
In vivo animal studies with citiolone are conducted in rodent models of liver injury, such as CCl4-induced hepatotoxicity or alcohol-induced liver damage. Animals are treated with citiolone at various doses, and liver function is assessed by measuring serum transaminases (ALT, AST), bilirubin, and histopathological examination of liver tissue. Markers of oxidative stress and inflammation are also measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for citiolone are limited. Its molecular weight is 159.2 g/mol. The compound is typically administered orally for liver therapy. Its absorption, distribution, metabolism, and excretion properties have not been extensively characterized. For research use, it is typically dissolved in suitable solvents.
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| Toxicity/Toxicokinetics |
Citiolone is generally well tolerated with a favorable safety profile. It has been studied in clinical trials up to Phase II with no significant adverse effects reported. The compound is considered safe for its intended use as a liver therapeutic. No significant organ toxicity has been reported.
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| Additional Infomation |
N-(2-oxo-3-thiacyclopentanoyl)acetamide is an N-acyl amino acid.
Citiolone is a hepatoprotective agent used for the treatment of liver disorders, including hepatitis and cirrhosis. It is a derivative of cysteine with antioxidant and mucolytic properties. The compound has been investigated in clinical trials up to Phase II. It is not approved by the FDA but is used in some countries as a liver therapeutic. |
| Molecular Formula |
C6H9NO2S
|
|---|---|
| Molecular Weight |
159.04
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| Exact Mass |
159.035
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| CAS # |
1195-16-0
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| PubChem CID |
14520
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| Appearance |
White to off-white solid powder
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| Density |
1.263 g/cm3
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| Boiling Point |
427.265ºC at 760 mmHg
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| Melting Point |
109-111ºC
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| Flash Point |
212.202ºC
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| LogP |
0.545
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
10
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| Complexity |
169
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
S1C(C([H])(C([H])([H])C1([H])[H])N([H])C(C([H])([H])[H])=O)=O
|
| InChi Key |
NRFJZTXWLKPZAV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H9NO2S/c1-4(8)7-5-2-3-10-6(5)9/h5H,2-3H2,1H3,(H,7,8)
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| Chemical Name |
N-(2-oxothiolan-3-yl)acetamide
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| Synonyms |
Citiolonum; Citiolona; Citiolase
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 100 mg/mL (~628.10 mM)
DMSO : ≥ 50 mg/mL (~314.05 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (15.70 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.38 mg/mL (14.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.2877 mL | 31.4386 mL | 62.8773 mL | |
| 5 mM | 1.2575 mL | 6.2877 mL | 12.5755 mL | |
| 10 mM | 0.6288 mL | 3.1439 mL | 6.2877 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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