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Lirimilast

Name: Lirimilast
Brand: TargetMol
SKU: T15766
Price: 183 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: BAY19-8004, BAY-19-8004, BAY 19-8004) Copy Product Info

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Synonyms: BAY19-8004, BAY-19-8004, BAY 19-8004

Catalog No. T15766 Copy Product Info

Purity: 99.68%

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Lirimilast (IC₅₀ = 49 nM) is a potent, selective, and orally active phosphodiesterase 4 (PDE4) inhibitor with significant anti-inflammatory effects, used in research on asthma and chronic obstructive pulmonary disease (COPD).

Cas No. 329306-27-6

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Pack Size	Price	USA Stock	Global Stock
1 mg	$183	-	In Stock
5 mg	$463	-	In Stock
10 mg	$787	-	In Stock
25 mg	$1,390	-	In Stock
50 mg	$1,980	-	In Stock
1 mL x 10 mM (in DMSO)	$497	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.68%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Lirimilast (IC₅₀ = 49 nM) is a potent, selective, and orally active phosphodiesterase 4 (PDE4) inhibitor with significant anti-inflammatory effects, used in research on asthma and chronic obstructive pulmonary disease (COPD).
Targets & IC50	PDE4:49 nM
In vitro	Methods: An in vitro PDE4 activity assay was conducted to compare the inhibitory potencies of Lirimilast, cilomilast and CDP‑840, using PDE4 freshly prepared from human PMNL as the enzyme source. Results: In the PDE4 assay, the potency of Lirimilast was approximately 5‑fold higher than that of cilomilast and comparable to that of CDP‑840 [1].
In vivo	Methods: Oral administration of Lirimilast and cilomilast was performed in pulmonary neutrophil inflammation models in guinea pigs, primates and rats to evaluate in vivo efficacy and therapeutic index. Results: The oral effective dose of Lirimilast was 3 mg/kg in guinea pigs and only 0.1 mg/kg per day in primates, showing a favorable therapeutic index. In the rat pulmonary neutrophil inflammation model, its potency was 3‑fold higher than that of cilomilast [2].
Synonyms	BAY19-8004, BAY-19-8004, BAY 19-8004

Chemical Properties

Molecular Weight	443.26
Formula	C₁₇H₁₂Cl₂N₂O₆S
Cas No.	329306-27-6
Smiles	O=C(N)NC1=C(OC=2C=C(OS(=O)(=O)C)C=CC21)C(=O)C3=CC=C(Cl)C=C3Cl
Relative Density.	1.619g/cm3

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: 80 mg/mL (180.48 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2560 mL	11.2801 mL	22.5601 mL	112.8006 mL
5 mM	0.4512 mL	2.2560 mL	4.5120 mL	22.5601 mL
10 mM	0.2256 mL	1.1280 mL	2.2560 mL	11.2801 mL
20 mM	0.1128 mL	0.5640 mL	1.1280 mL	5.6400 mL
50 mM	0.0451 mL	0.2256 mL	0.4512 mL	2.2560 mL
100 mM	0.0226 mL	0.1128 mL	0.2256 mL	1.1280 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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.