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Mapracorat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mapracorat图片
CAS NO:887375-26-0
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Mapracorat 是一种新型非甾体选择性糖皮质激素受体激动剂。
Cas No.887375-26-0
别名ZK-245186; BOL-303242X
Canonical SMILESCC(C)(C1=C(OCC2)C2=CC(F)=C1)C[C@@](O)(CNC3=C4C=CC(C)=NC4=CC=C3)C(F)(F)F
分子式C25H26F4N2O2
分子量462.48
溶解度DMSO : ≥ 50.6 mg/mL (109.41 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.

Mapracorat concentration dependently inhibited TNFα secretion from activated canine PBMC with IC50 value of approximately 0.2 nM.

Intradermal injection of compound 48/80 (50 ug in 50 uL saline) resulted in a clear wheal and flare reaction over the 60 min observation period. Topical pre-treatment with mapracorat (0.1%) and triamcinolone acetonide (0.015%) led to significant reduction in the wheal and flare responses compared to vehicle (acetone) treated areas. However, once daily topical administration of triamcinolone acetonide significantly reduced skin fold thickness from day 8 to 14, whereas no such reduction was observed for mapracorat.

References:
[1]. Baumer W , et al. The selective glucocorticoid receptor agonist mapracorat displays a favourable safety-efficacy ratio for the topical treatment of inflammatory skin diseases in dogs. Vet Dermatol. 2017 Feb; 28(1):46-e11.
[2]. Baiula M, et al. Mapracorat, a novel non-steroidal selective glucocorticoid receptor agonist for the treatment of allergic conjunctivitis.Inflamm Allergy Drug Targets. 2014; 13(5):289-98.