CI-1044 (PD-189659) (Synonyms: PD-189659) |
Catalog No.GC31786 |
CI-1044 (PD-189659) 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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 197894-84-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [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. |
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 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].
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].
[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.
Cas No. | 197894-84-1 | SDF | |
Synonyms | PD-189659 | ||
Canonical SMILES | O=C(C1=CC=CN=C1)N[C@H]2C(N3C4=C(CC3)C=C(N)C=C4C(C5=CC=CC=C5)=N2)=O | ||
Formula | C23H19N5O2 | M.Wt | 397.43 |
Solubility | DMSO : 125 mg/mL (314.52 mM) | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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