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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $297 | 8-10 weeks | |
25 mg | $987 | 8-10 weeks | |
50 mg | $1,360 | 8-10 weeks | |
100 mg | $1,860 | 8-10 weeks | |
1 mL x 10 mM (in DMSO) | $318 | 8-10 weeks |
Description | CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3). |
Targets&IC50 | PDE4D3:0.09 μM, PDE4C2:0.56 μM, PDE4A5:0.29 μM, PDE4B2:0.08 μM |
In vitro | CI-1044 selectively inhibits PDE4 crude extract from U937 cells (IC50: 0.27 μM). It being threefold more potent than rolipram (IC50=0.91 μM) and tenfold less potent than cilomilast (IC50=0.026 μM) in the same assay. For CI-1044, cilomilast and rolipram, the production of TNF-α is dose-dependently decreased with mean IC50 values from three separate experiments of 0.31±0.05, 0.26±0.05 and 0.11±0.01 μM, respectively, in the presence of PDE4 inhibitors. |
In vivo | CI-1044 dose-dependently inhibits the accumulation of eosinophils in Bronchoalveolar lavages (BAL) fluids (ID50: 3.25 mg/kg). CI-1044 (p.o.) plasma levels increase proportionally with doses ranging between 0.1 and 40 mg/kg. Following repeated administration with CI-1044( p.o.), the ID50 value represents 0.5 mg/kg. TNF-α production is dose-dependently inhibited by CI-1044, rolipram, and cilomilast (ID50s: 0.4, 1.4, and 1.6 mg/kg) following single oral administration. A single dose treatment with CI-1044 (10 mg/kg, p.o.) 24, 8, 3, or 1 h before the antigen challenge induces 6, 56, 48, and 79% inhibition in the number of eosinophils in BAL. |
Alias | PD-189659 |
Molecular Weight | 397.43 |
Formula | C23H19N5O2 |
Cas No. | 197894-84-1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 125 mg/mL (314.52 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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