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| 25mg |
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Purity: ≥98%
Cilomilast (also known as SB-207,499; SB207499; trade name Ariflo) is a novel, potent and orally bioactive phosphodiesterase 4/PDE4 inhibitor with potential anti-inflammatory and immunomodulatory activity. It inhibits PDE4 with an IC50 of ~110 nM, it has anti-inflammatory activity and low central nervous system activity. It has the potential to be used for the treatment of asthma and chronic obstructive obstructive pulmonary (COPD).
| ln Vitro |
Human neutrophil functions are inhibited by cipolast (0.1 nM–10 μM; 5 min)[2]. A 5-minute exposure to cipomalost (0.1 nM–10 μM) inhibits the eosinophil chemiluminescence response[2]. Cilomilast (0.001-100 μM; 30 min) prevents human monocytes and human whole blood from synthesizing TNFα[2].
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| ln Vivo |
In mice, SB-207499 (1-100 mg/kg; po) substantially and dose-dependently suppresses human TNFα production[1]. With an ED50 of 2.3 mg/kg, SB-207499 (0.1-100 mg/kg; oral gavage) restores reserpine-induced hypothermia in mice[1]. In mice, intralesional IL-4 concentrations and the chronic oxazolone-induced inflammatory response are inhibited by SB-207499 (500 μg/ear; bid for 6 d)[1].
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| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse (18-25 g) are injected with human monocytes and LPS[1]
Doses: 1, 5, 10, 50, 100 mg/kg Route of Administration: Po after the injection of human monocytes and before LPS challenge Experimental Results: Inhibited the production of human TNFα, with an ED50 of 4.9 mg/kg. |
| References |
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| Additional Infomation |
4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)-1-cyclohexanecarboxylic acid is a member of methoxybenzenes.
Cilomilast (Ariflo, SB-207,499) is a drug which was developed for the treatment of respiratory disorders such as asthma and Chronic Obstructive Pulmonary Disease (COPD). It is orally active and acts as a selective Phosphodiesterase-4 inhibitor. Following four clinical trials, the drug proved to be effective in treating COPD, however it has never been marketed due to a poor side effect profile. Drug Indication Investigated for use/treatment in chronic obstructive pulmonary disease (COPD). Mechanism of Action Cilomilast shows high selectivity for cAMP-specific PDE4, an isoenzyme that predominates in pro-inflammatory and immune cells and that is 10-fold more selective for PDE4D than for PDE4A, -B or -C. In vitro, cilomilast suppresses the activity of several pro-inflammatory and immune cells that have been implicated in the pathogenesis of asthma and COPD. Moreover, it is highly active in animal models of these diseases. Cilomilast has been shown to exert potent anti-inflammatory effects both in vitro and in vivo. |
| Molecular Formula |
C20H25NO4
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| Molecular Weight |
343.42
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| Exact Mass |
343.178
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| CAS # |
153259-65-5
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| Related CAS # |
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| PubChem CID |
151170
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
549.1±50.0 °C at 760 mmHg
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| Melting Point |
157ºC
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| Flash Point |
285.9±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.568
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
511
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CFBUZOUXXHZCFB-LDTOLXSISA-N
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| InChi Code |
InChI=1S/C20H25NO4/c1-24-17-7-6-15(12-18(17)25-16-4-2-3-5-16)20(13-21)10-8-14(9-11-20)19(22)23/h6-7,12,14,16H,2-5,8-11H2,1H3,(H,22,23)/t14-,20+
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| Chemical Name |
cis-4-Cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid
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| Synonyms |
Cilomilast; SB 207499; SB207499; Ariflo; SB-207499;
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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: ≥ 2.5 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO+95% Corn oil:30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9119 mL | 14.5594 mL | 29.1189 mL | |
| 5 mM | 0.5824 mL | 2.9119 mL | 5.8238 mL | |
| 10 mM | 0.2912 mL | 1.4559 mL | 2.9119 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00103922 | Completed | Drug: cilomilast | Pulmonary Disease, Chronic Obstructive | GlaxoSmithKline | November 2004 | Phase 3 |
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