AZD-0284
目录号: PL11075 纯度: ≥99%
CAS No. :2101291-07-8
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中文名称
AZD-0284
英文名称
AZD-0284
英文别名
AZD-0284;(R)-2-acetyl-N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-5-(methylsulfonyl)isoindoline-1-carboxamide;C(C)(=O)N1[C@H](C2=CC=C(C=C2C1)S(=O)(=O)C)C(=O)NC1=CC=C(C=C1)C(C(F)(F)F)(C(F)(F)F)O;5G4XF6VU2Y;AZD0284;(1~{R})-2-ethanoyl-~{N}-[4-[1,1,1,3,3,3-hexakis(fluoranyl)-2-oxidanyl-propan-2-yl]phenyl]-5-methylsulfonyl-1,3-dihydroisoindole-1-carboxamide;GTPL11711;BDBM50575029;AT10695;compound 20 [PMID: 34464130];(1R)-2-acetyl-N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-5-methylsulfonyl-1,3-dihydroisoindole-1-carboxamide;(R)-2-acetyl-N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan;Unii-5G4XF6VU2Y
Cas No.
2101291-07-8
分子式
C21H18F6N2O5S
分子量
524.43
包装储存
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
AZD-0284 是选择性的核受体 (RORγ) 的选择性反向激动剂。AZD-0284 具有用于斑块型寻常型银屑病和呼吸道疾病的潜力。
生物活性
AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment.
性状
Solid
IC50 & Target[1][2]
pIC50: 7.4 (FRET RORγ)
体外研究(In Vitro)
AZD0284 (0.37 μM; 5 days) inhibits IL-17A production in human TH17 cells.
AZD0284 reduces polarization of TH17 into pathogenic TH17/1 cells. AZD0284 decreases frequency of single IL-17cell as well as double positive TH17/1 cells. AZD0284 reduces IL-17A secretion and RNA expression of IL-17A, IL-17F, IL-22 and IL-23R. 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
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
ClinicalTrial
参考文献
[1]. Narjes, F, et al. The discovery of AZD0284, an inverse agonist of the nuclear receptor RORg. American Chemical Society, 2017 Drug Design and Delivery Symposium 26 October 2017
[2]. Asimus S, et al. Pharmacokinetics, pharmacodynamics and safety of the inverse retinoic acid-related orphan receptor γ agonist AZD0284 [published online ahead of print, 2020 Feb 17]. Br J Clin Pharmacol. 2020;10.1111/bcp.14253.
溶解度数据
In Vitro: DMSO : 100 mg/mL (190.68 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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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