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CI-1044

Catalog No. T14962Cas 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).

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

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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).
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.
Alias	PD-189659

Chemical Properties

Molecular Weight	397.43
Formula	C23H19N5O2
Cas No.	197894-84-1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (314.52 mM)

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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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