Dagrocorat (Synonyms: PF-00251802)
目录号: PL04649 纯度: ≥99%
CAS No. :1044535-52-5
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中文名称
Dagrocorat
中文别名
(4bS,7R,8aR)-4b-benzyl-7-hydroxy-N-(2-methylpyridin-3-yl)-7-(trifluoromethyl)-5,6,8,8a,9,10-hexahydrophenanthrene-2-carboxamide
英文名称
Dagrocorat
英文别名
Dagrocorat;OPM23UN90U;Dagrocorat [USAN:INN];Fagrocorat;Dagrocorat (USAN/INN);PF 0251802;PF 00251802;GTPL9650;US8901310, Example 1;BDBM140009;AOB87471;DB14676;D10617;Q27285777;(4bS,7R,8aR)-4b-benzyl-7-hydroxy-N-(2-methylpyridin-3-yl)-7-(trifluoromethyl)-
Cas No.
1044535-52-5
分子式
C29H29F3N2O2
分子量
494.55
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Dagrocorat (PF-00251802) 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 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 可用于类风湿性关节炎的研究。
生物活性
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC 50 =1.3 μM in human liver microsomes) and CYP2D6 (K i =0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis.
性状
Solid
IC50 & Target[1][2]
IC50: 1.3 μM (CYP3A in human liver microsomes); IC50: 0.57 μM (CYP2D6 in human liver microsomes)
体外研究(In Vitro)
Dagrocorat is metabolized by cytochrome P450 (CYP)3A to an N-oxide metabolite. Dagrocorat is a reversible inhibitor of several CYPs, such as CYP3A and CYP2D6. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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 Mar;7(3):244-255.
溶解度数据
In Vitro: DMSO : 250 mg/mL (505.51 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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