Diacerein
Based on 7 publication(s) in Google Scholar
Diacerein (Diacerhein), an orally active anthraquinone, reduces production of IL-1 converting enzyme then inhibits the activation of IL-1β by related downstream signaling. Diacerein is an anti-inflammatory and anti-rheumatic drug. Diacerein can relieve bronchospasm and control airway inflammation in asthmatic mice. Diacerein has the potential for slow acting drug in osteoarthritis (SYSADOA) research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.64%
- CAS. Nr.: 13739-02-1
- Formel: C19H12O8
- Molecular Weight:368.29
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Diacerein
More- Br J Cancer. 2024 Jul;131(2):231-242. [Abstract]
- Cell Rep. 2025 May 14;44(5):115712. [Abstract]
- Ecotoxicol Environ Saf. 2023 Aug:261:115130. [Abstract]
- Biochem Pharmacol. 2026 Jan 24:247:117748. [Abstract]
- Biochem Pharmacol. 2025 May:235:116819. [Abstract]
- Molecules. 2026 Mar 5;31(5):864. [Abstract]
- J Inflamm Res. 2024 Nov 19:17:9071-9085. [Abstract]
Alle Calcium Channel Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
IL-1β |
L-type calcium channel |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | CC50 |
108.2 μM
Compound: Diacerein
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Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
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[PMID: 34491054] |
| RAW264.7 | IC50 |
106.9 μM
Compound: Diacerein
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Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-6 production incubated for 48 hrs by ELISA analysis
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-6 production incubated for 48 hrs by ELISA analysis
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[PMID: 34491054] |
| RAW264.7 | IC50 |
126.77 μM
Compound: Diacerein
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Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in TNF-alpha production incubated for 48 hrs by ELISA analysis
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in TNF-alpha production incubated for 48 hrs by ELISA analysis
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[PMID: 34491054] |
| RAW264.7 | IC50 |
65.41 μM
Compound: Diacerein
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Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-1beta production incubated for 48 hrs by ELISA analysis
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-1beta production incubated for 48 hrs by ELISA analysis
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[PMID: 34491054] |
In Vitro
Diacerein (Diacerhein; 30-300 μM; 24, 48 h) reduces cell proliferation and viability of chondrosarcoma cells[1].
Diacerine (30-300 μM; 48 h) causes a SW-1353 cell cycle G2/M arrest[1].
Diacerein (30-300 μM; 48 h) decreases cyclin B1, CDK1, and CDK2 levels in SW-1353 cell[1].
Diacerein can relax the agonist-precontracted mouse airway smooth muscle via intracellular and extracellular calcium mobilization which is mediated by switched voltage-dependent L-type Ca2+ channels, non-selective cation channels, large-conductance Ca2+-activated K+ channel, and Na+/Ca2+ exchangers[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Cal-78 and SW-1353 cells
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Concentration:30, 100, and 300 μM
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Incubation Time:24, 48 h
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Result:Inhibited cell growth in a concentration dependent manner in both cell lines.
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Cell Line:Cal-78 and SW-1353 cells
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Concentration:30, 100, and 300 μM
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Incubation Time:48 h
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Result:Caused a pronounced decrease in the number of cells in the G1 phase, accompanied by a significant increase of the number of S and G2/M phase cells, indicating a G2/M arrest in SW-1353 cells.
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Cell Line:Cal-78 and SW-1353 cells
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Concentration:30, 100, and 300 μM
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Incubation Time:24 h
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Result:Induced a small, but not significant change, for the expression of CDK1, whereas the cyclin B1 and CDK2 levels were significantly down-regulated in the case of Cal-78 cells.
In Vivo
Diacerein (2, 20, 60 mg/kg; daily; oral; at 2 weeks of age transgenic mice; for 5 weeks) reveales a significant reduction not only in cartilage destruction but also in the extent of synovitis and bone erosion in the Tg197 transgenic murine model of RA[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice at 6-8 weeks of age[2]
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Dosage:50, 100, 200 mg/kg
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Administration:Gavaged; daily; a week
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Result:Reduced systematic inflammation and mucus secretion in vivo.
Exhibited anti-inflammatory property to significantly reduce inflammation and repair damaged airway.
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. 13739-02-1
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Appearance Solid
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Molecular Weight 368.29
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Formel C19H12O8
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Color Light yellow to yellow
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SMILES
O=C(C(C=C1C2=O)=CC(OC(C)=O)=C1C(C3=C2C=CC=C3OC(C)=O)=O)O
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Synonyms
Diacerhein; Diacetylrhein
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (7)
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Journal Impact Factor
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Most Recent
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Br J Cancer
PARP inhibition leads to synthetic lethality with key splicing-factor mutations in myelodysplastic syndromes. [Abstract]2024 Jul;131(2):231-242. PMID: 38806724 -
Cell Rep
Septo-subicular cholinergic circuit promotes seizure development via astrocytic inflammation. [Abstract]2025 May 14;44(5):115712. PMID: 40372911 -
Ecotoxicol Environ Saf
Factors ameliorate pro-inflammatory microglia polarization through inhibition of reactive astrocytes induced by 2-chloroethanol. [Abstract]2023 Aug:261:115130. PMID: 37311391 -
Biochem Pharmacol
Diacerein protects against Ovariectomy-Induced bone loss via reversal of NRF2 epigenetic suppression. [Abstract]2026 Jan 24:247:117748. PMID: 41587594 -
Biochem Pharmacol
FTO aggravates podocyte injury and diabetic nephropathy progression via m6A-dependent stabilization of ACC1 mRNA and promoting fatty acid metabolism. [Abstract]2025 May:235:116819. PMID: 39988261 -
Molecules
2026 Mar 5;31(5):864. PMID: 41828851 -
J Inflamm Res
Interleukin 1β Mediates the Pathogenesis of Nasal Mucosal Epithelial Barrier Dysfunction in Allergic Rhinitis. [Abstract]2024 Nov 19:17:9071-9085. PMID: 39588138
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 12.5 mg/mL (33.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (283 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)
Verweise
[1]. Birgit Lohberger, et al. Diacerein retards cell growth of chondrosarcoma cells at the G2/M cell cycle checkpoint via cyclin B1/CDK1 and CDK2 downregulation. BMC Cancer. 2015 Nov 10:15:891. [Content Brief]
[2]. Shi S, Xue L, Han S, et al. Anti-Contractile and Anti-Inflammatory Effects of Diacerein on Isolated Mouse Airways Smooth Muscle and Mouse Asthma Model. Front Pharmacol. 2020;11:560361. [Content Brief]
[3]. Eleni Douni, et al. Attenuation of inflammatory polyarthritis in TNF transgenic mice by diacerein: comparative analysis with dexamethasone, methotrexate and anti-TNF protocols. Arthritis Res Ther. 2004;6(1):R65-R72. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7153 mL | 13.5763 mL | 27.1525 mL | 67.8813 mL |
| 5 mM | 0.5431 mL | 2.7153 mL | 5.4305 mL | 13.5763 mL | |
| 10 mM | 0.2715 mL | 1.3576 mL | 2.7153 mL | 6.7881 mL | |
| 15 mM | 0.1810 mL | 0.9051 mL | 1.8102 mL | 4.5254 mL | |
| 20 mM | 0.1358 mL | 0.6788 mL | 1.3576 mL | 3.3941 mL | |
| 25 mM | 0.1086 mL | 0.5431 mL | 1.0861 mL | 2.7153 mL | |
| 30 mM | 0.0905 mL | 0.4525 mL | 0.9051 mL | 2.2627 mL |
Diacerein Related Classifications
HY-N0283 Related Classifications
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