Rosiptor(Synonyms: AQX-1125)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Rosiptor (Synonyms: AQX-1125) 纯度: ≥98.0%

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。

Rosiptor(Synonyms: AQX-1125)

Rosiptor Chemical Structure

CAS No. : 782487-28-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4510 In-stock
5 mg ￥4100 In-stock
10 mg ￥5900 In-stock
25 mg ￥10000 In-stock
50 mg ￥14000 In-stock
100 mg   询价  
200 mg   询价  

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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[1][2].

IC50 & Target

SHIP1[1]
体外研究
(In Vitro)

Rosiptor (0.1-10 μM; 30 minutes) inhibits Akt activation in MOLT-4, but not in Jurkat cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MOLT-4 cells and SHIP1-deficient Jurkat cells (IGF-1 stimulation)
Concentration: 0.1, 1, 10 μM
Incubation Time: 30 minutes
Result: Induced a concentration-dependent decrease in Akt phosphorylation in MOLT-4 cells, while it failed to affect Akt phosphorylation in Jurkat cells.

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[2].
Rosiptor (10 mg/kg; p.o.) has the Cmax value of 0.830 μM and the t1/2 value of 5.2 hours. AQX-1125 also exhibits >80% oral bioavailability[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 weeks old male CD-1 mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: p.o.; daily for 3 days
Result: Significantly reduced the total number of BAL leukocytes in NSC-125066-challenged mice, up to a maximum of 60% at 7 days and 63% at 21 days at 30 mg/kg; Reduced MPO activity by 54% at Day 7 and by 74% at Day 21 at 30 mg/kg.
Animal Model: Male Sprague-Dawley rats[1]
Dosage: 10 mg/kg (Pharmacokinetic Study)
Administration: Oral administration
Result: The Cmax value is 0.830 μM and the t1/2 value is 5.2 hours.

Clinical Trial

分子量

321.50

Formula

C20H35NO2
CAS 号

782487-28-9
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 150 mg/mL (466.56 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1104 mL 15.5521 mL 31.1042 mL
5 mM 0.6221 mL 3.1104 mL 6.2208 mL
10 mM 0.3110 mL 1.5552 mL 3.1104 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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