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Bioactivity of PF-4136309

Description PF-4136309 is a highly effective, selective, oral CCR2 antagonist capable of inhibiting CCR2 in humans, mice, and rats with IC50 values of 5.2 nM, 17 nM, and 13 nM, respectively.

Related category

Signal path > > G protein coupled receptor /G protein > > CCR

Signal path > > Immunity and Inflammation > > CCR

Research Field > > Inflammation/immunity

target

Human CCR2:5.2 nM (IC50)

Mouse CCR2:13 nM (IC50)

Rat CCR2:17 nM (IC50)

In vitro studies of PF-4136309 were effective in human chemotactic activity (IC50 = 3.9nM) and in whole blood assays (IC50 = 19nM), and in mouse and rat chemotactic assays IC50 was 16 and 2.8nM. PF-4136309 effectively inhibits CCr2-mediated signaling events, such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation, with IC50 values of 3.3 and 0.5nM respectively. In hERG patch clamp determination, PF-4136309 inhibited hERG potassium current with IC50 of 20μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, and the IC50 value of five major CYP isoenzymes: CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 > 30μM. In addition, PF-4136309 is not a CYP inducer with concentrations up to 30μM [1].

In vivo studies PF-4136309 (2mg/kg) showed a moderate half-life in both species after intravenous administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10mg/kg) is rapidly absorbed with a peak concentration time (Tmax) of 1.2 hours in rats and 0.25 hours in dogs. Similar half-lives were observed in both species between iv administration and po administration. PF-4136309 was well absorbed and the oral bioavailability of both species was 78% [1].

Reference literature

[1]. Xue CB, et al. Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist. ACS Med. Chem. Lett., 2011, 2 (12), pp 913-918.

Physical and chemical properties of PF-4136309

Molecular formula C29H31F3N6O3

Molecular weight 568.59000

Accurate mass 568.24100

PSA 120.34000

LogP 4.02780