Cilomilast (SB-207499) is among the first of a new generation of PDE4 inhibitors (Ki ≈100 nM). Cilomilast (SB-207499)inhibits HPDE4 and LPDE4 catalytic activity with equal potency (Ki ≈100 nM). SB-207499 and rolipram are equipotent against LPDE4, but cilomilast (SB-207499) is 100-fold less potent against HPDE4. This profile suggests that cilomilast (SB-207499) retain the anti-inflammatory activity of rolipram yet have a decreased tendency to produce side effects.
| Cell Experiment | |
|---|---|
| Cell lines | U937 cells |
| Preparation method | Incubating U937 cells (1-2 × 106) at 37 °C in a shaking water bath with Cilomilast for 1 min before the addition of 0.1 μM PGE2 (total volume of 200 μL). The incubation proceeds for an additional 4 min and is stopped by the addition of 0.1 mL of HClO4 (17.5%), neutralized with 0.15 ml of K23 (1.0 M) and diluted to 1 mL with sodium acetate buffer. Centrifuging the samples at 3000 × g for 10 min. Assaying aliquots of the supernatant fraction for cAMP content by radioimmunoassay using commercially available kits. |
| Concentrations | 0.1-10 μM |
| Incubation time | 5 min |
| Animal Experiment | |
|---|---|
| Animal models | Balb/c, CD-1 and C57B1/6 male mice weighing from 18 to 25 g with human monocytes or endotoxin-induced shock |
| Formulation | Olive oil |
| Dosages | 3, 6, 12, 25, 50 mg/kg |
| Administration | Gavage |
| Molecular Weight | 343.42 |
| Formula | C20H25NO4 |
| CAS Number | 153259-65-5 |
| Solubility (25°C) | DMSO 59 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Stephen Rennard, et al. The efficacy and safety of cilomilast in COPD
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