Rosiptor - CAS:782487-28-9

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Rosiptor (Synonyms:AQX-1125)

目录号 : KM4607 CAS No. : 782487-28-9 纯度 : ≥98%

Data Sheet 产品使用指南

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。

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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.

体外研究

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

Western Blot Analysis

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

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.

Animal Model:	6-8 weeks old male CD-1 mice
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
Dosage:	10 mg/kg (Pharmacokinetic Study)
Administration:	Oral administration
Result:	The C_max value is 0.830 μM and the t_1/2 value is 5.2 hours.

分子式

C₂₀H₃₅NO₂

分子量

321.50

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。

临床试验

科研文献

•Cell Biol Int. 2020 Dec 15.

纯度： ≥98%

Data Sheet

产品使用指南

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