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CI-1044

Name: CI-1044
Brand: TargetMol
SKU: T14962
Rating: 4.5 (1 reviews)

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Catalog No. T14962Cas No. 197894-84-1

Alias 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).

CI-1044

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Catalog No. T14962Alias PD-189659Cas No. 197894-84-1

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

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$297	8-10 weeks	8-10 weeks
25 mg	$987	8-10 weeks	8-10 weeks
50 mg	$1,360	8-10 weeks	8-10 weeks
100 mg	$1,860	8-10 weeks	8-10 weeks
1 mL x 10 mM (in DMSO)	$318	8-10 weeks	8-10 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

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	PDE4B2:0.08 μM, PDE4D3:0.09 μM, PDE4C2:0.56 μM, PDE4A5:0.29 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

Chemical Properties

Molecular Weight	397.43
Formula	C₂₃H₁₉N₅O₂
Cas No.	197894-84-1
Smiles	Nc1cc2CCN3c2c(c1)C(=N[C@@H](NC(=O)c1cccnc1)C3=O)c1ccccc1
Relative Density.	1.43 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

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

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (8.3 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5162 mL	12.5808 mL	25.1617 mL	125.8083 mL
5 mM	0.5032 mL	2.5162 mL	5.0323 mL	25.1617 mL
10 mM	0.2516 mL	1.2581 mL	2.5162 mL	12.5808 mL
20 mM	0.1258 mL	0.6290 mL	1.2581 mL	6.2904 mL
50 mM	0.0503 mL	0.2516 mL	0.5032 mL	2.5162 mL
100 mM	0.0252 mL	0.1258 mL	0.2516 mL	1.2581 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc