(Rac)-PF-184 hydrate

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本产品不向个人销售，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。

包装:	5mg
市场价:	5454元

产品介绍

(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

产品描述

(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 T_1/2of 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 µM; 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 µL, 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.