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Ensifentrine

Name: Ensifentrine
Brand: TargetMol
SKU: T25376
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T25376Cas No. 1884461-72-6

Alias Ensifentrinum, Ensifentrina

Ensifentrine (Ensifentrinum) is a PDE3/4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis.

Ensifentrine

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Purity: 99.94%

Catalog No. T25376Alias Ensifentrinum, EnsifentrinaCas No. 1884461-72-6

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$89	In Stock	In Stock
10 mg	$146	In Stock	In Stock
25 mg	$297	In Stock	In Stock
50 mg	$476	In Stock	In Stock
100 mg	$762	In Stock	In Stock
200 mg	$987	-	In Stock
1 mL x 10 mM (in DMSO)	$98	In Stock	In Stock

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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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Batch Information

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Purity:99.94%

Appearance:Solid

Color:White to Green

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	Ensifentrine (Ensifentrinum) is a PDE3/4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis.
Targets&IC50	PDE4:1479 nM, PDE3:0.4 nM
In vitro	Electrical field stimulation-induced contraction of guinea pig superfused isolated tracheal preparations was significantly inhibited by Ensifentrine (10 microM) (percentage control; 93 +/- 1.2). Contractile responses were suppressed for up to 12 h after termination of superfusion with Ensifentrine demonstrating a long duration of action. Ensifentrine4 inhibited, in a concentration-dependent manner, lipopolysaccharide-induced tumor necrosis factor alpha release from human monocytes [IC50; 0.52 microM (0.38-0.69)] and proliferation of human mononuclear cells to phytohemagglutinin [IC50; 0.46 microM (0.24-0.9)][2].
In vivo	Ensifentrine administered orally significantly inhibited eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs. Likewise, inhalation of dry powder containing Ensifentrine by conscious guinea pigs (25% in micronized lactose) 1.5 h before antigen exposure significantly inhibited the recruitment of eosinophils to the airways. Exposure of conscious guinea pigs to inhalation of dry powder containing Ensifentrine (2.5%) and RPL565 (25%) in micronized lactose significantly inhibited histamine-induced plasma protein extravasation in the trachea and histamine-induced bronchoconstriction over a 5.5-h period[2].
Synonyms	Ensifentrinum, Ensifentrina

Chemical Properties

Molecular Weight	477.56
Formula	C₂₆H₃₁N₅O₄
Cas No.	1884461-72-6
Smiles	COc1cc2CCn3c(c\c(=N/c4c(C)cc(C)cc4C)n(CCNC(N)=O)c3=O)-c2cc1OC
Relative Density.	1.29 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 16.33 mg/mL (34.19 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.09 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	2.0940 mL	10.4699 mL	20.9398 mL	104.6989 mL
5 mM	0.4188 mL	2.0940 mL	4.1880 mL	20.9398 mL
10 mM	0.2094 mL	1.0470 mL	2.0940 mL	10.4699 mL
20 mM	0.1047 mL	0.5235 mL	1.0470 mL	5.2349 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