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Cilomilast

Cat. No. M3437

Cilomilast Structure

Synonym: SB-207499

Size Price Availability
5mg USD 90 1-2 Weeks
10mg USD 160 1-2 Weeks
50mg USD 520 1-2 Weeks
200mg USD 1200 1-2 Weeks
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 343.42
Formula C20H25NO4
CAS Number 153259-65-5
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Cilomilast, SB-207499 supplier, PDE, inhibitors

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