(Rac)-PF-184 hydrate_product_DataBase

Bioactivity

(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[1].

Invitro

(Rac)-PF-184 has slow dissociation kinetics with a T1/2 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[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].

In Vivo

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

Name

(Rac)-PF-184 hydrate

Formula

C32H34ClFN6O5

Molar Mass

659.64

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Sommers CD, et al. Novel tight-binding inhibitory factor-kappaB kinase (IKK-2) inhibitors demonstrate target-specific anti-inflammatory activities in cellular assays and following oral and local delivery in an in vivo model of airway inflammation. J Pharmacol Exp Ther. 2009 Aug;330(2):377-88.

PeptideDB

(Rac)-PF-184 hydrate

CAS: F: C32H34ClFN6O5 W: 659.64