Cilomilast
Cilomilast
CAS: 153259-65-5
Molecular Formula: C20H25NO4
Cilomilast - Names and Identifiers
| Name | Cilomilast |
| Synonyms | CS-515 Clomilast Cilomilast CILOMILAST Cilomilast, SB 207499, Ariflo 4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)-1-cyclohexanecarboxylic acid 4-cyano-4-(3-cyclopentyloxy-4-methoxy-phenyl)cyclohexane-1-carboxylic acid |
| CAS | 153259-65-5 |
| EINECS | 200-258-5 |
| InChIKey | CFBUZOUXXHZCFB-OYOVHJISSA-N |
Cilomilast - Physico-chemical Properties
| Molecular Formula | C20H25NO4 |
| Molar Mass | 343.42 |
| Density | 1.21±0.1 g/cm3(Predicted) |
| Melting Point | 157°C |
| Boling Point | 549.1±50.0 °C(Predicted) |
| Solubility | DMSO: soluble15mg/mL, clear |
| Appearance | powder |
| Color | white to beige |
| pKa | 4.45±0.25(Predicted) |
| Storage Condition | -20°C |
| In vitro study | Cilomilast acts on U937 cells to increase cAMP content, and this effect is concentration-dependent. When Cilomilast and (R)-rolipram inhibited LPS-induced TNF-α formation in isolated human monocytes, the effect was similar, with an IC50 of 7.0 and 7.2, respectively. Both Cilomilast and (R)-rolipram moderately inhibited fMLP-induced degranulation of human neutrophils. Cilomilast and (R)-rolipram inhibited neutrophil activity with similar effects, with IC50 values of 7.1 and 6.4, respectively. |
| In vivo study | In Vivo, Cilomilast inhibits human TNFα production with an ED50 of 4.9 mg/kg. Cilomilast is as effective as R-rolipram when inhibiting TNFα production, but when used to treat reserpine-induced hypothermia, Cilomilast (ED50 of 2.3 mg/kg, P. O.) it is 10 times less effective than R-rolipram (ED50 of 0.23 mg/kg, oral). In a time-course study, Cilomilast (30 mg/kg, P. O.) inhibited TNFα production for at least 10 H. The ability of Cilomilast to regulate interleukin-4 production in vivo was evaluated in a chronic oxazolone-induced contact-sensitive model in Balb/c mice. Local treatment of Cilomilast(1000 μg) inhibited the damaging concentration of interleukin-4. |
Cilomilast - Risk and Safety
| WGK Germany | 3 |
Cilomilast - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.912 ml | 14.559 ml | 29.119 ml |
| 5 mM | 0.582 ml | 2.912 ml | 5.824 ml |
| 10 mM | 0.291 ml | 1.456 ml | 2.912 ml |
| 5 mM | 0.058 ml | 0.291 ml | 0.582 ml |
Last Update：2024-01-02 23:10:35
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