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PF-4136309

CAS No. : 1341224-83-6

MCE 站：PF-4136309

产品活性：PF-4136309 是一种高效，选择性，可口服的 CCR2 拮抗剂，能够抑制人，小鼠和大鼠 CCR2，IC₅₀ 值分别为 5.2 nM，17 nM 和 13 nM。

研究领域：GPCR/G Protein  |  Immunology/Inflammation

作用靶点：CCR

In Vitro: PF-4136309 is potent in human chemotaxis activity (IC₅₀=3.9 nM) and in the whole blood assay (IC₅₀=19 nM), with IC₅₀ of 16 and 2.8 nM in mouse and rat chemotaxis assays. PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation with IC₅₀ values of 3.3 and 0.5 nM, respectively. In hERG patch clamp assay, PF-4136309 inhibits hERG potassium current with an IC₅₀ of 20 μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, with IC₅₀ values of >30 μM against five major CYP isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Moreover, PF-4136309 is not a CYP inducer at concentrations up to 30 μM.

In Vivo: PF-4136309 (2 mg/kg) exhibits a moderate half-life in both species after iv administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10 mg/kg) is absorbed rapidly, with peak concentration time (T_max) at 1.2 h for rats and 0.25 h for dogs. A similar half-life is observed in both species between iv dosing and po dosing. PF-4136309 is well absorbed, with an oral bioavailability of 78% in both species.

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