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(Rac)-PF-184 hydrate

CAS No. :

MCE 站：(Rac)-PF-184 hydrate

产品活性：(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。

研究领域：NF-κB

作用靶点：IKK

In Vitro: (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 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.
(Rac)-PF-184 inhibits LPS-induced cytokine production from rat alveolar macrophages ａnd blocked p65 nuclear translocation.

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

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