(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。
| 生物活性 | (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]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | (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 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].
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体内研究
(In Vivo) | (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. |
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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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