Rosiptor (Synonyms: AQX-1125)
目录号: PL09582 纯度: ≥98.0%
CAS No. :782487-28-9
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中文名称
Rosiptor
中文别名
索马鲁肽
英文名称
Rosiptor
英文别名
Rosiptor;6R5034F862;(1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexan-1-ol;(1S,3S,4R)-4-[(3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methylidene-3,3a,4,5,6,7-hexahydro-2H-inden-5-yl]-3-(hydroxymethyl)-4-methylcyclohexan-1-ol;Rosiptor [USAN];Rosiptor (USAN/INN);GTPL9249;AQX1125;AQX 1125;DB13012
Cas No.
782487-28-9
分子式
C20H35NO2
分子量
321.50
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Rosiptor (AQX-1125) 是一种选择性,具有口服活性的磷酸酶 SHIP1 激活剂,具有抗炎作用。Rosiptor (AQX-1125) 在体外抑制 Akt 磷酸化、炎症介质生成和白细胞趋化。
生物活性
Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
性状
Solid
IC50 & Target[1][2]
SHIP1
体外研究(In Vitro)
Rosiptor (0.1-10 μM; 30 minutes) inhibits Akt activation in MOLT-4, but not in Jurkat cells. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot AnalysisCell Line
体内研究(In Vivo)
Rosiptor (3-30 mg/kg; p.o.; daily for 3 days) significantly reduces the total number of BAL leukocytes in NSC-125066-challenged mice and reduces MPO activity.
Rosiptor (10 mg/kg; p.o.) has the C max value of 0.830 μM and the t 1/2 value of 5.2 hours. AQX-1125 also exhibits >80% oral bioavailability. 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
ClinicalTrial
参考文献
[1]. Stenton GR, et al. Characterization of AQX-1125, a small-molecule SHIP1 activator: Part 1. Effects on inflammatory cell activation and chemotaxis in vitro and pharmacokinetic characterization in vivo. Br J Pharmacol. 2013 Mar;168(6):1506-18.
[2]. Cross J, et al. AQX-1125, small molecule SHIP1 activator inhibits NSC-125066-induced pulmonary fibrosis. Br J Pharmacol. 2017 Sep;174(18):3045-3057.
溶解度数据
In Vitro: DMSO : 150 mg/mL (466.56 mM; Need ultrasonic and warming)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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