CP-195543

CP-195543 is a potent, selective and orally active leukotriene B4 (LTB4) receptor antagonist with IC50s of 6.8, 37.0 nM for human neutrophils and murine spleen membranes, respectively. CP-195543 blocks CD11b up-regulation. CP-195543 inhibits LTB4-mediated neutrophil infiltration[1].

Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor

Research Areas >> Inflammation/Immunology

LTB4

CP-195543 抑制由 LTB4 介导的人和小鼠中性粒细胞趋化性，IC50 值分别为 2.4 nM、7.5 nM[1]。 CP-195543 (0.1 nM-10 µM；60 分钟) 阻断人中性粒细胞 (HN) 和小鼠中性粒细胞中 CD11b 的上调，对人单核细胞和嗜酸性粒细胞的 IC50 值分别为 270、420 nM [1]。

CP-195543 (0.01, 0.1, 1, 10 mg/kg for guinea pig; 0.01, 0.1, 1, 10, 100 mg/kg for mice; P.o.; 1 h before injection of LTB4) 呈剂量依赖性抑制 LTB4 介导的中性粒细胞浸润[1]。 Animal Model: Guinea pig (Injection of LTB4 10, 30, 100 ng/site; injected intradermally)[1] Dosage: 0.01, 0.1, 1, 10 mg/kg Administration: P.o.; 1 h before injection of LTB4 Result: Inhibited LTB4-mediated neutrophil infiltration in guinea pigskin in a dose-dependent manner. Animal Model: Mice (Injection of LTB4 100 ng/site; injected intradermally)[1] Dosage: 0.01, 0.1, 1, 10, 100 mg/kg Administration: P.o.; 1 h before injection of LTB4 Result: Inhibited LTB4-mediated neutrophil infiltration in guinea pigskin in a dose-dependent manner.

[1]. Showell HJ, et al. The preclinical pharmacological profile of the potent and selective leukotriene B4 antagonist CP-195543. J Pharmacol Exp Ther. 1998 Jun;285(3):946-54.