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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.
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 | TNFα secretion (canine PBMCs):0.2 nmol/L, TNFα 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]. |
Alias | ZK-245186, ZK245186, BOL-303242X, BOL303242X |
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 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (64.87 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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