(Rac)-PF-184 hydrate|西域试剂

(Rac)-PF-184 hydrate,98.0%

产品编号：Bellancom-107591A| 分子式：C₃₂H₃₄ClFN₆O₅| 分子量：659.64

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-107591A		￥2050.00	杭州北京（现货）
Bellancom-107591A		￥6060.00	杭州北京（现货）

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(Rac)-PF-184 hydrate

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。

生物活性

(Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC₅₀ of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects.

体外研究

(Rac)-PF-184 has slow dissociation kinetics with a T_1/2 of 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.
(Rac)-PF-184 binds tightly to endogenous IKK-2 and shows extended inhibition of kinase activity and cytokine production.
(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.
(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.
(Rac)-PF-184 inhibits LPS-induced cytokine production from rat alveolar macrophages and blocked p65 nuclear translocation.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
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 EC₅₀ values of 1 mg. Dose-dependently suppressed BAL fluid TNF- and PGE2 levels comparable with cell infiltration. Inhibited p65 translocation. Showed long-lasting activity.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
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 EC₅₀ values of 1 mg. Dose-dependently suppressed BAL fluid TNF- and PGE2 levels comparable with cell infiltration. Inhibited p65 translocation. Showed long-lasting activity.