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(Rac)-PF-184 hydrate
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
(Rac)-PF-184 hydrate图片
包装: 5mg
市场价: 5454元

半岛bd体育手机客户端 介绍
(Rac)-PF-184 hydrate 是一种有效的 inhibitory factor-κB kinase 2 (IKK-2) 抑制剂，IC50 值为 37 nM。(Rac)-PF-184 hydrate 具有抗炎作用。
分子式 C32H34ClFN6O5
分子量 659.64
储存条件 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
半岛bd体育手机客户端 描述

(Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with anIC50of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects[1].

(Rac)-PF-184 has slow dissociation kinetics with a T1/2of 6.7 h from rhIKK-2, very low oral bioavailability (5%), high intravenous clearance (59 ml/min/kg), and high P450 metabolism in human liver microsomes[1].
(Rac)-PF-184 binds tightly to endogenous IKK-2 and shows extended inhibition of kinase activity and cytokine production[1].
(Rac)-PF-184 shows a concentration-dependent inhibition on LPS- and IL-1β-induced production of inflammatory mediators in a variety of human disease-relevant cells[1].
(Rac)-PF-184 (0.001-10 ?M; 1 h) inhibits IL-1β-induced TNF-α in a concentration-dependent manner with maximal efficacies of 94% and relative potencies of 163 nM[1].
(Rac)-PF-184 inhibits LPS-induced cytokine production from rat alveolar macrophages and blocked p65 nuclear translocation[1].

(Rac)-PF-184 (0.3-2.5 mg; i.t.; once) blocks neutrophil infiltration and BAL cell cytokine production[1].

Animal Model: Fasted male Sprague-Dawley rats (350 g) placed into a chamber connected to a large volume nebulizer filled with 20 ml of 1 mg/mL solution of LPS[1]
Dosage: 0.3-2.5 mg
Administration: Nano suspension and administered intratracheally in a volume of 100 ?L, 60 min before aerosolized LPS
Result: Resulted in a comparable attenuation of total cell and PMN cell infiltration 4 h after LPS exposure. Dose-dependently inhibited cell infiltration with EC50values of 1 mg. Dose-dependently suppressed BAL fluid TNF- and PGE2 levels comparable with cell infiltration. Inhibited p65 translocation. Showed long-lasting activity.

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