| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Dovramilast targets phosphodiesterase 4 (PDE4), an enzyme that specifically breaks down cyclic AMP (cAMP). By inhibiting PDE4, the compound increases intracellular cAMP levels. Elevated cAMP leads to the activation of protein kinase A (PKA) and the subsequent inhibition of pro-inflammatory signaling pathways. This results in the reduced production of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-12.
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| ln Vitro |
In vitro, Dovramilast inhibits PDE4 activity and reduces the production of pro-inflammatory mediators and cytokines. Specific IC50 values for PDE4 inhibition are not provided in the available sources. Its activity has been demonstrated in various cell-based assays measuring cytokine production.
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| ln Vivo |
Dolflast (oral gavage, 5, 25, or 50 mg/kg as a single dosage) dramatically improves antibiotic-mediated bacterial killing and lowers lung pathology [2]. Pharmacokinetic characteristics of dolfast in B6D2F1 mice [2]. Sampling time (h) Concentration (ng/ml) CC-11050 only CC-11050+INH 1 1,331.6±136.97 905.35±594.23 2 1,409.47±140.85 1,309.39±214.08 5 948.85±128.7 1,609.18±1 6 7.2 8 820.6±265.98 1,271.73±249.18 24 1.27 ±1.1 4.96±1.85 Tmax(h) 2.0 5.0 Cmax(ng/ml) 1,410 1,610 AUClast(ng × h/ml) 10,200 13,900
In vivo, Dovramilast reduces inflammation and improves isoniazid-mediated bacterial clearance from the lungs. This suggests it could be a valuable adjunct therapy for tuberculosis, helping to reduce the inflammatory damage caused by the infection while improving the efficacy of standard antibiotic treatment. It is also being studied for lupus erythematosus. |
| Enzyme Assay |
A cell-free assay for Dovramilast would involve measuring its inhibition of PDE4 enzymatic activity. Recombinant PDE4 is incubated with a cAMP substrate in the presence of varying concentrations of the compound. The amount of cAMP hydrolyzed is measured, and the IC50 is calculated. Specific IC50 values are not provided in the available sources.
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| Cell Assay |
Cellular assays for Dovramilast typically involve measuring its effects on cytokine production in immune cells. Cells, such as PBMCs, are treated with the compound and stimulated with a pro-inflammatory stimulus. The production of cytokines like TNF-α, IL-6, and IL-12 is measured by ELISA or other immunoassays. The compound's ability to reduce cytokine production confirms its anti-inflammatory activity.
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| Animal Protocol |
Animal/Disease Models: B6D2F1 mice[2]
Doses: 5, 25 or 50 mg/kg given Medication method: oral administration, 5, 25 or 50 mg/kg, single dose. Experimental Results: The expression of PDE4 in the lungs of MTB-infected mice was diminished. Animal/Disease Models: B6D2F1 mice [2] Doses: 5, 25 or 50 mg/kg Route of Administration: po (oral gavage), 5, 25 or 50 mg/kg, single dose Experimental Results: Improved antibiotic-mediated bacterial killing and Reduce lung pathology. In vivo animal experiments for Dovramilast have been conducted in models of tuberculosis. The compound's ability to reduce inflammation and improve bacterial clearance when combined with isoniazid has been demonstrated. Specific protocols and data are not detailed in the available sources. |
| ADME/Pharmacokinetics |
Dovramilast is an orally active compound. Specific pharmacokinetic parameters, such as half-life and bioavailability, are not provided in the available sources. The compound is being developed for oral administration.
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| Toxicity/Toxicokinetics |
Toxicity data for Dovramilast are not detailed in the available sources. As an investigational drug, its safety profile is being established. It is intended for research use and is not for human consumption.
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| References | |
| Additional Infomation |
CC-11050 is being studied in the clinical trial NCT01300208 (evaluating the preliminary safety, tolerability, pharmacokinetics, pharmacodynamics and efficacy of CC-11050 in patients with discoid lupus erythematosus and subacute cutaneous lupus erythematosus).
Dovramilast (CAS: 340019-69-4) is an orally active PDE4 inhibitor. It is also known as CC-11050. The compound reduces the production of pro-inflammatory mediators and cytokines. It is being studied as a host-directed therapy for pulmonary tuberculosis and for the treatment of lupus erythematosus. It is not an approved drug and is strictly for research purposes. |
| Molecular Formula |
C24H28N2O6S
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|---|---|
| Molecular Weight |
472.55
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| Exact Mass |
472.166
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| CAS # |
340019-69-4
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| PubChem CID |
10322579
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
823
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(C(NC2=CC=CC3=C2C(=O)N([C@@H](C2=CC=C(OC)C(OCC)=C2)CS(C)(=O)=O)C3)=O)CC1
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| InChi Key |
QDZOBXFRIVOQBR-LJQANCHMSA-N
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| InChi Code |
InChI=1S/C24H28N2O6S/c1-4-32-21-12-16(10-11-20(21)31-2)19(14-33(3,29)30)26-13-17-6-5-7-18(22(17)24(26)28)25-23(27)15-8-9-15/h5-7,10-12,15,19H,4,8-9,13-14H2,1-3H3,(H,25,27)/t19-/m1/s1
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| Chemical Name |
N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-3-oxo-1H-isoindol-4-yl]cyclopropanecarboxamide
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : ~25 mg/mL (~52.90 mM)
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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 | 2.1162 mL | 10.5809 mL | 21.1618 mL | |
| 5 mM | 0.4232 mL | 2.1162 mL | 4.2324 mL | |
| 10 mM | 0.2116 mL | 1.0581 mL | 2.1162 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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