| Size | Price | Stock | Qty |
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| 500mg |
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| 1g | |||
| Other Sizes |
Purity: ≥98%
Diacerein ( Diacerhein; Diacetylrhein) is slow-acting medication which acts as a potent inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, it is indicated for osteoarthritis and chronic inflammatory arthritis. Diacerein significantly inhibits LPS-induced IL-1beta production by synovial tissue and cartilage. Diacerein (1 μM) has a significantly less inhibitory effect on cartilage synthesis than culture media containing LPS only.
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| Animal Protocol |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Bioavailability is 50-60%. It is completely converted to the active metabolite emodin [DB13174] before entering systemic circulation. Estimated in rats, 37% is excreted in the urine and 53% in the feces. Volume: 15-60 L. Total clearance: 1.5 L/h; renal clearance: 0.1 L/h. Metabolism/Metabolite Before entering systemic circulation, it is completely converted to emodin [DB13174] via double deacetylation. Emodin [DB13174] is further metabolized to emodin glucuronide and emodin sulfate. Biological Half-Life 4-10 hours. |
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| Toxicity/Toxicokinetics |
Protein Binding
99% of emodin binds to plasma proteins. |
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| References |
Osteoarthritis Cartilage.1999 May;7(3):272-80;Osteoarthritis Cartilage.1999 May;7(3):255-64.
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| Additional Infomation |
4,5-Diaacetoxy-9,10-dioxo-2-anthracarboxylic acid is an anthraquinone compound. Diacerein is a prodrug that is metabolized to emodin. Currently, diacerein is approved in France for the treatment of osteoarthritis, but its use is limited due to its side effects, including severe diarrhea. Diacerein is being investigated for the treatment of insulin resistance, type 2 diabetes, and its complications. Drug Indications For the treatment of osteoarthritis of the hip or knee. Mechanism of Action The active metabolite of diacerein, emodin [DB13174], reduces cartilage destruction by decreasing the expression of matrix metalloproteinases (MMPs)-1 and -3, and by upregulating the expression of tissue inhibitors of matrix metalloproteinases (TIMPs), which can reduce the activity of multiple MMPs. The anti-inflammatory effects of emodin can reduce the activity level of interleukin-1β, which plays an important role in reducing extracellular matrix production, MMP activity, and persistent inflammation. Emodin reduces the synthetic activity of abnormal osteoblasts through an unknown mechanism.
Pharmacodynamics Reduces inflammation and cartilage destruction, and corrects abnormal osteoblast activity. |
| Molecular Formula |
C19H12O8
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|---|---|---|
| Molecular Weight |
368.29
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| Exact Mass |
368.053
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| CAS # |
13739-02-1
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| Related CAS # |
Diacerein-d6;1325559-27-0
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| PubChem CID |
26248
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
631.5±55.0 °C at 760 mmHg
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| Melting Point |
217-2180C
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| Flash Point |
231.8±25.0 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.634
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| LogP |
1.99
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
683
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
TYNLGDBUJLVSMA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H12O8/c1-8(20)26-13-5-3-4-11-15(13)18(23)16-12(17(11)22)6-10(19(24)25)7-14(16)27-9(2)21/h3-7H,1-2H3,(H,24,25)
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| Chemical Name |
4,5-diacetyloxy-9,10-dioxoanthracene-2-carboxylic acid
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (13.58 mM) in 1% (w/v) carboxymethylcellulose (CMC) (add these co-solvents sequentially from left to right, and one by one), suspension solution.
Solubility in Formulation 2: 1%CMC Na : 30mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7153 mL | 13.5763 mL | 27.1525 mL | |
| 5 mM | 0.5431 mL | 2.7153 mL | 5.4305 mL | |
| 10 mM | 0.2715 mL | 1.3576 mL | 2.7153 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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