| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Citreorosein targets multiple inflammatory signaling pathways. It is a cAMP phosphodiesterase inhibitor. It inhibits proinflammatory cytokine production through inhibition of both MAPKs and AKT-mediated IκB kinase (IKK) phosphorylation and subsequent inhibition of transcription factor NF-κB activation. Citreorosein also attenuates cyclooxygenase-2-dependent prostaglandin D2 generation by blocking Akt and JNK pathways in mouse bone marrow-derived mast cells. It inhibits the nuclear translocation of NF-κB p65 subunit and its DNA-binding activity.
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|---|---|
| ln Vitro |
In vitro, citreorosein exhibits potent and broad-spectrum antibacterial activity against Gram-positive bacteria. It attenuates degranulation and LTC4 generation through suppression of multiple step signaling pathways, which would be beneficial for the prevention of allergic inflammation. Citreorosein inhibits COX-2-dependent prostaglandin D2 generation by blocking Akt and JNK pathways in mouse bone marrow-derived mast cells. It also inhibits the nuclear translocation of NF-κB p65 subunit and its DNA-binding activity.
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| ln Vivo |
In vivo, citreorosein represents a potential therapeutic approach for the treatment of inflammatory diseases. Its anti-inflammatory effects have been demonstrated in mouse models, where it attenuates allergic inflammation through suppression of multiple signaling pathways. The compound's ability to inhibit NF-κB activation and COX-2-dependent prostaglandin production suggests potential for treating inflammatory conditions. However, detailed in vivo efficacy data are limited.
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| Enzyme Assay |
In vitro enzyme assays for citreorosein typically involve measuring its inhibition of cAMP phosphodiesterase, MAPKs, AKT, IKK, and COX-2. The compound is incubated with the enzyme of interest in the presence of substrate, and enzyme activity is measured using appropriate assays (e.g., phosphodiesterase activity using colorimetric or fluorescence-based methods; kinase activity using radioactive or luminescent assays; COX-2 activity using prostaglandin production assays). Binding to NF-κB can be assessed using DNA-binding or electrophoretic mobility shift assays.
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| Cell Assay |
In vitro cell-based assays for citreorosein involve culturing appropriate cell lines (e.g., mast cells, macrophages) and treating them with the compound to assess effects on inflammatory responses. Mast cells are sensitized and stimulated with antigen to measure degranulation and LTC4 production. Macrophages are stimulated with LPS to measure cytokine production. NF-κB activation is assessed by measuring nuclear translocation of p65 or by reporter gene assays. Cell viability is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies for citreorosein have been conducted in mouse models of allergic inflammation. Mice are sensitized and challenged with an allergen, and citreorosein is administered orally or intraperitoneally to assess inhibition of allergic responses. Inflammatory markers, including cytokine levels, cell infiltration, and histopathology, are evaluated. Standard protocols for allergic inflammation models are employed. No standardized protocol is available.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of citreorosein have not been extensively characterized. As an anthraquinone derivative, it is expected to have moderate oral bioavailability. Anthraquinones are typically metabolized in the liver by cytochrome P450 enzymes and undergo glucuronidation and sulfation. The compound may have a relatively long half-life due to its polycyclic structure. No specific PK data are available.
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| Toxicity/Toxicokinetics |
The toxicity profile of citreorosein has not been systematically evaluated. Anthraquinones can exhibit cytotoxicity and genotoxicity at high concentrations, and some anthraquinones are known to be carcinogenic. However, citreorosein's specific toxicity profile has not been characterized. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available.
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| References | |
| Additional Infomation |
Citreorosein is a trihydroxyanthraquinone. It has been reported to be found in Hamigra aviranene, Tararomyces isla, and other organisms with relevant data.
Citreorosein is a naturally occurring anthraquinone derivative with anti-inflammatory and antibacterial activities. It is a cAMP phosphodiesterase inhibitor that inhibits NF-κB activation through inhibition of MAPKs and AKT-mediated IKK phosphorylation. The compound attenuates COX-2-dependent prostaglandin D2 generation by blocking Akt and JNK pathways. Citreorosein is a research compound with potential applications in inflammatory disease research. It is not approved for clinical use. |
| Molecular Formula |
C15H10O6
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|---|---|
| Molecular Weight |
286.24
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| Exact Mass |
286.047
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| CAS # |
481-73-2
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| PubChem CID |
361512
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
672.3±55.0 °C at 760 mmHg
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| Melting Point |
288 °C
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| Flash Point |
374.4±28.0 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.783
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| LogP |
3.38
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
449
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OCC1C=C(O)C2C(C3C(O)=CC(O)=CC=3C(=O)C=2C=1)=O
|
| InChi Key |
YQHZABGPIPECSQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10O6/c16-5-6-1-8-12(10(18)2-6)15(21)13-9(14(8)20)3-7(17)4-11(13)19/h1-4,16-19H,5H2
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| Chemical Name |
1,3,8-trihydroxy-6-(hydroxymethyl)anthracene-9,10-dione
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4936 mL | 17.4679 mL | 34.9357 mL | |
| 5 mM | 0.6987 mL | 3.4936 mL | 6.9871 mL | |
| 10 mM | 0.3494 mL | 1.7468 mL | 3.4936 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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