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CI-1044

Catalog No. T14962   CAS 197894-84-1
Synonyms: PD-189659

CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3).

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CI-1044 Chemical Structure
CI-1044, CAS 197894-84-1
Pack Size Availability Price/USD Quantity
5 mg 8-10 weeks $ 297.00
25 mg 8-10 weeks $ 987.00
50 mg 8-10 weeks $ 1,360.00
100 mg 8-10 weeks $ 1,860.00
1 mL * 10 mM (in DMSO) 8-10 weeks $ 318.00
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage & Solubility Information
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 PDE4C2:0.56 μM, PDE4A5:0.29 μM, PDE4B2:0.08 μM, PDE4D3:0.09 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.
Synonyms 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

Solubility Information

DMSO: 125 mg/mL (314.52 mM), sonification is recommended.

TargetMolReferences and Literature

1. Pruniaux MP, et al. Relationship between phosphodiesterase type 4 inhibition and anti-inflammatory activity of CI-1044 in rat airways. Fundam Clin Pharmacol. 2010 Feb;24(1):73-82.

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Keywords

CI-1044 197894-84-1 Metabolism PDE PD 189659 CI 1044 PD189659 PD-189659 CI1044 inhibitor inhibit

 

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