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Dagrocorat hydrochloride
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。
Dagrocorat hydrochloride图片
CAS NO:1044535-61-6
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Dagrocorat (PF-00251802) hydrochloride 是一种具有口服活性,选择性和高亲和性部分糖皮质激素受体的激动剂。Dagrocorat hydrochloride 也是一种时间依赖性可逆抑制剂,对 CYP3A (IC50=1.3 μM) 和CYP2D6 (Ki=0.57 μM) 有抑制作用。Dagrocorat hydrochloride 可用于类风湿性关节炎的研究。
Cas No.1044535-61-6
别名PF-00251802 hydrochloride
分子式C29H30ClF3N2O2
分子量531.01
溶解度DMSO : 100 mg/mL (188.32 mM; ultrasonic and warming and heat to 60℃)
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

Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis[1].

Dagrocorat hydrochloride is metabolized by cytochrome P450 (CYP)3A to an N-oxide metabolite. Dagrocorat hydrochloride is a reversible inhibitor of several CYPs, such as CYP3A and CYP2D6[1].

[1]. Ripp SL, et al. In Vitro and In Vivo Investigation of Potential for Complex CYP3A Interaction for PF-00251802 (Dagrocorat), a Novel Dissociated Agonist of the Glucocorticoid Receptor. Clin Pharmacol Drug Dev. 2018;7(3):244-255.