Cilomilast (Synonyms: SB 207499) |
Catalog No.GC17598
One-Click Copy Product Info
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A PDE4 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 153259-65-5
Sample solution is provided at 25 µL, 10mM.
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Cilomilast, also known as SB-207499 or Ariflo, is a potent second generation inhibitor of type 4 phosphodiesterase (PDE4), an enzyme metabolizing cellular cyclic adenosine monophosphate (cAMP) which acts as a second messenger to disrupt the function of inflammatory cell and induce airway smooth muscle relaxation. Cilomilast is currently used for the treatment of chronic obstructive pulmonary disease (COPD) due to its strong anti-inflammatory activity as well as inhibitory effects against the release of neutrophil chemoattractants (such as tumor necrosis factor TNF- α, interleukin IL-8 and granulocyte-macrophage colony stimulating factor GM-CSF) and suppression of the recruitment of neutrophils into tissues and the LTB4 production.
Reference
[1].M Profita, G Chiappara, F Mirabella, RCDi Giorgi, L Chimenti, G Costanzo, L Riccobono, V Bellia, J Bousquet, and A M Vignola. Effect of cilomilast (Ariflo) on TNF-α, IL-8, and GM-CSF release by airway cells of patients with COPD. Thorax 2003; 58: 573-579
[2].Barry D. Zussman, Lisa J. Benincosa, Dawn M Webber, David j. Clark, Hugh Cowley, John Kelly, Robert D. Murdoch, James Upward, Peter Wyld, Andreas Port and Hermann Fuder. An overview of the pharmacokinetics of cilomilast (Ariflo), a new, orally active phosphodiesterase 4 inhibitor, in healthy young and elderly volunteers. J Clin Pharmacol 2001; 41: 950-958
| Cell experiment [1]: | |
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Cell lines |
MCS cell lines |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
11 d; 40 μM |
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Applications |
The results demonstrate that inhibition of PDE (Cilomilast) enhances ALP expression in MSCs via the cAMP pathway. The increase in the level of ALP activity is dependent on the dose of cilomilast. To study the effect of the inducers on MSC differentiation at similar proliferation rates, we treated MCSs, except those cultured in osteogenic medium, with 1% DMSO. We compared MSCs cultured for 11 days in the presence of different inducers with MSCs cultured in osteogenic medium in order to quantify the osteogenetic effects of the inducers. We found that the ALP activity levels of MCSs treated with a combination of PDE4 inhibitor (40 μM) and BMP-2 (300 ng/mL) were almost double the ALP activity level of MSCs treated with osteogenic medium, suggesting that the mineralisation process is more rapid. |
| Animal experiment [2]: | |
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Animal models |
Female C57BL/6 mice |
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Dosage form |
Cilomilast 0.05%; ocular surface instillation three times per day over a period of 7 days. |
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Applications |
Real-time PCR was used to quantify the expression of transcripts encoding IL-1α, IL-1β, and TNF-α in the corneas and conjunctivae of DED-induced mice. Treatment with topical cilomilast significantly decreased the corneal expression of TNF-α as compared with the vehicle-treated group. Compared with the DED-untreated corneas, treatment with cilomilast significantly reduced IL-1α and TNF-α expression. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Munisso M C, Kang J H, Tsurufuji M, et al. Cilomilast enhances osteoblast differentiation of mesenchymal stem cells and bone formation induced by bone morphogenetic protein 2[J]. Biochimie, 2012, 94(11): 2360-2365. [2] Sadrai Z, Stevenson W, Okanobo A, et al. PDE4 inhibition suppresses IL-17–associated immunity in dry eye disease[J]. Investigative ophthalmology & visual science, 2012, 53(7): 3584-3591. | |
| Cas No. | 153259-65-5 | SDF | |
| Synonyms | SB 207499 | ||
| Chemical Name | 4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexane-1-carboxylic acid | ||
| Canonical SMILES | COC1=C(C=C(C=C1)C2(CCC(CC2)C(=O)O)C#N)OC3CCCC3 | ||
| Formula | C20H25NO4 | M.Wt | 343.42 |
| Solubility | ≥ 12.95 mg/mL in DMSO, ≥ 49.9 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9119 mL | 14.5594 mL | 29.1189 mL |
| 5 mM | 582.4 μL | 2.9119 mL | 5.8238 mL |
| 10 mM | 291.2 μL | 1.4559 mL | 2.9119 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)