CI-1044 is an orally active PDE4 inhibitor with IC 50 s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5 , PDE4B2 , PDE4C2 and PDE4D3 , respectively. In Vitro CI-1044 is an orally active PDE4 inhibitor with IC 50 s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively. CI-1044 selectively inhibits PDE4 crude extract from U937 cells with an IC 50 value of 0.27±0.02 μM being threefold more potent than rolipram (IC 50 =0.91±0.14) and tenfold less potent than cilomilast (IC 50 =0.026±0.007) in the same assay. In the presence of PDE4 inhibitors, the production of TNF-α is dose dependently decreased with mean IC 50 values from three separate experiments of 0.31±0.05, 0.26±0.05 and 0.11±0.01 μM, for CI-1044, cilomilast and rolipram, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo TNF-α production is dose-dependently inhibited by CI-1044, rolipram and cilomilast with ID 50 s of 0.4, 1.4 and 1.6 mg/kg respectively following single oral administration. Following repeated administration with CI-1044, the ID 50 value represents 0.5 mg/kg p.o.. CI-1044 plasma levels increase proportionally with doses ranging between 0.1 and 40 mg/kg p.o. (R2=0.878). CI-1044 dose dependently inhibits the accumulation of eosinophils in Bronchoalveolar lavages (BAL) fluids with an ID 50 value of 3.25 mg/kg. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:PDE4A5 0.29 μM (IC 50 ) PDE4B2 0.08 μM (IC 50 ) PDE4C2 0.56 μM (IC 50 ) PDE4D3 0.09 μM (IC 50 )
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CI-1044
CAS number：197894-84-1 molecular formula：C23H19N5O2
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Specs
| Chinese alias | - | ||
| English alias | SCHEMBL6441242 | BDBM50473083 | N-(9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro(1,4)diazepino(6,7,1-hi)indol-3-yl)nicotinamide | AKOS040741548 | CI-1044 | Q27285326 | (R)-N-(9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-3-yl)nicotin | ||
| CAS number | 197894-84-1 | molecular formula | C23H19N5O2 |
| molecular weight | 397.43 g/mol | Exact mass | ≥98% |
| PSA | 101.000 Ų | logp | 2.000 |
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