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Mapracorat

Name: Mapracorat
Brand: TargetMol
SKU: T13451L
Rating: 4.5 (1 reviews)

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Catalog No. T13451LCas No. 887375-26-0

Alias ZK-245186, ZK245186, BOL-303242X, BOL303242X

Mapracorat (ZK-245186, BOL-303242X) is a selective glucocorticoid receptor agonist commonly used as an anti-inflammatory agent for atopic dermatitis, post-cataract surgery inflammation, and allergic conjunctivitis.

Mapracorat

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Catalog No. T13451LAlias ZK-245186, ZK245186, BOL-303242X, BOL303242XCas No. 887375-26-0

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Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	Mapracorat (ZK-245186, BOL-303242X) is a selective glucocorticoid receptor agonist commonly used as an anti-inflammatory agent for atopic dermatitis, post-cataract surgery inflammation, and allergic conjunctivitis.
Targets&IC50	TNF-α secretion (canine PBMCs):0.2 nmol/L, TNF-α secretion (murine BMDCs):0.5 nmol/L
In vitro	The in vitro activity of mapracorat was evaluated in canine peripheral blood mononuclear cells (PBMCs) and murine bone marrow–derived dendritic cells (BMDCs). Cells were pretreated with mapracorat (0.1–100 nmol/L) for 30 minutes, then stimulated with lipopolysaccharide (1 μg/mL) and incubated for 24 hours. TNFα levels in the supernatant were measured by ELISA. Mapracorat dose-dependently inhibited TNFα secretion, with IC₅₀ values of approximately 0.2 nmol/L (canine PBMCs) and 0.5 nmol/L (murine BMDCs) [1].
In vivo	The in vivo activity of mapracorat was assessed in a canine skin inflammation model. Beagle dogs received topical applications of 0.1% mapracorat (500 μL in acetone) on shaved skin areas, once daily for four doses. One hour after the final application, compound 48/80 (50 μg/50 μL) was intradermally injected to induce wheal and erythema. Mapracorat significantly reduced both wheal and erythema size, comparable to 0.015% triamcinolone acetonide [1].
Synonyms	ZK-245186, ZK245186, BOL-303242X, BOL303242X

Chemical Properties

Molecular Weight	462.48
Formula	C₂₅H₂₆F₄N₂O₂
Cas No.	887375-26-0
Smiles	C(C[C@@](CNC=1C2=C(C=CC1)N=C(C)C=C2)(C(F)(F)F)O)(C)(C)C3=C4C(=CC(F)=C3)CCO4
Relative Density.	no data available

Storage & Solubility Information

Storage

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: 30 mg/mL (64.87 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1623 mL	10.8113 mL	21.6226 mL	108.1128 mL
5 mM	0.4325 mL	2.1623 mL	4.3245 mL	21.6226 mL
10 mM	0.2162 mL	1.0811 mL	2.1623 mL	10.8113 mL
20 mM	0.1081 mL	0.5406 mL	1.0811 mL	5.4056 mL
50 mM	0.0432 mL	0.2162 mL	0.4325 mL	2.1623 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.

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

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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