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 activephosphataseSHIP1activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibitsAktphosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro[1][2]. |
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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].
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. |
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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 Cmaxvalue of 0.830 μM and the t1/2value of 5.2 hours. AQX-1125 also exhibits >80% oral bioavailability[1].
| 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 Cmaxvalue is 0.830 μM and the t1/2value is 5.2 hours. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 150 mg/mL(466.56 mM;Need ultrasonic and warming) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
