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  • Rosiptor (AQX-1125)
Rosiptor (AQX-1125)的可视化放大

Rosiptor (AQX-1125)

Rosiptor (AQX-1125) (AQX-1125) 是一种具有抗炎作用的选择性和口服活性磷酸酶 SHIP1 激活剂。 Rosiptor (AQX-1125) (AQX-1125) 在体外抑制 Akt 磷酸化、炎症介质产生和白细胞趋化性。

原价
¥4425-34700
价格
3540-27760
Rosiptor (AQX-1125)的二维码

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  • 货号: ajce49808
  • CAS: 782487-28-9
  • 别名: 罗西普托,AQX-1125
  • 分子式: C20H35NO2
  • 分子量: 321.5
  • 纯度: >98%
  • 溶解度: DMSO : 150 mg/mL (466.56 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

Rosiptor is an activator of SH2-containing inositol-5'-phosphatase 1 (SHIP1).


Rosiptor is a small-molecule SHIP1 activator.The activating effect of Rosiptor on SHIP1 is 28% at 100 μM in the native enzyme but no effect of Rosiptor is observed when the SHIP1δC2 enzyme is used. Rosiptor induces a concentration-dependent decrease in Akt phosphorylation in MOLT-4 cells, while it fails to affect Akt phosphorylation in Jurkat cells. At 0.1 μM Rosiptor the inhibition amounts to an average of 34%, while at 10 μM the inhibition amounts to an average of 82% in two independent experiments. Rosiptor also induces a concentration-dependent decrease in the production of multiple pro-inflammatory mediators in this system, without affecting cell viability. Rosiptor dose dependently inhibits chemotaxis of most cell types at low micromolar concentrations independent of the chemotactic stimulus[1].


In female Sprague-Dawley rats, the single-dose pharmacokinetics of Rosiptor show that the increases in maximal plasma concentration (Cmax) and AUC0-∞ are dose-proportional at the lower end of the dosing regimen and greater than dose proportional at the higher doses. The oral bioavailability of Rosiptor in rats is 66 and 85% at 10 and 30 mg/kg respectively. Oral bioavailability of Rosiptor in dogs is 88 and 104% at 10 and 30 mg/kg respectively. High tissue concentrations of Rosiptor are detected, as compared to plasma concentrations, at each time point studied[1].


[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.

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