1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

CI-1044 (Synonyms: PD-189659)

Cat. No.: HY-100246 Purity: 98.00%
Handling Instructions

CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively.

For research use only. We do not sell to patients.

CI-1044 Chemical Structure

CI-1044 Chemical Structure

CAS No. : 197894-84-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 788 In-stock
Estimated Time of Arrival: December 31
1 mg USD 563 In-stock
Estimated Time of Arrival: December 31
5 mg USD 901 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1442 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively.

IC50 & Target

PDE4A5

0.29 μM (IC50)

PDE4B2

0.08 μM (IC50)

PDE4C2

0.56 μM (IC50)

PDE4D3

0.09 μM (IC50)

In Vitro

CI-1044 is an orally active PDE4 inhibitor with IC50s 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 IC50 value of 0.27±0.02 μM being threefold more potent than rolipram (IC50=0.91±0.14) and tenfold less potent than cilomilast (IC50=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 IC50 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[1].

In Vivo

TNF-α production is dose-dependently inhibited by CI-1044, rolipram and cilomilast with ID50s of 0.4, 1.4 and 1.6 mg/kg respectively following single oral administration. Following repeated administration with CI-1044, the ID50 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 ID50 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[1].

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (314.52 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5162 mL 12.5808 mL 25.1617 mL
5 mM 0.5032 mL 2.5162 mL 5.0323 mL
10 mM 0.2516 mL 1.2581 mL 2.5162 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

References
Cell Assay
[1]

Blood from anesthetized rats is collected in heparin tubes, immediately distributed in 96-well microplates (250 μL/well) and incubated for 30 min at 37°C/5% CO2. Twenty-five microliters of vehicle or increasing concentrations of CI-1044, rolipram, cilomilast or solvant (saline/DMSO<0.1%) are added in wells and incubated for 30 min before the addition of LPS (100 μg/mL) or saline. Plasma is removed after a 22 to 24 h incubation at 37°C/5% CO2, transferred in another 96-well microplate and stored at ) -80°C until a TNF-α assay by ELISA[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Male rats (200 to 220 g) are used and receive either vehicle or CI-1044 orally at 0.4, 1, 4, 10 and 40 mg/kg. In the single administration experiment, all treatments are given 1 h before blood collection. In the repeated administration experiment, the treatments are given twice a day during 13 days and once on day 14, 1 h before blood sampling[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

397.43

Formula

C₂₃H₁₉N₅O₂

CAS No.

197894-84-1

SMILES

O=C(C1=CC=CN=C1)N[[email protected]]2C(N3C4=C(CC3)C=C(N)C=C4C(C5=CC=CC=C5)=N2)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
CI-1044
Cat. No.:
HY-100246
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CI-1044

Cat. No.: HY-100246