產(chǎn)品目錄

規(guī)格	10mM*1mLinDMSO 5mg 10mg 50mg 100mg
CAS	782487-28-9
別名	N/A
化學名	N/A
分子式	C20H35NO2
分子量	321.5
溶解度	DMSO : 150 mg/mL (466.56 mM)
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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