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 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.|
|Incubation time||5 min|
|Animal models||Balb/c, CD-1 and C57B1/6 male mice weighing from 18 to 25 g with human monocytes or endotoxin-induced shock|
|Dosages||3, 6, 12, 25, 50 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 59 mg/mL|
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