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编 号：F251977
分子式：C24H19F3O4
分子量：428.4
分子式：C24H19F3O4
分子量：428.4
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CAS No: 204981-48-6
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生物活性：
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.
体内研究：
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。Animal Model:Guinea pig (Injection of LTB4 10, 30, 100 ng/site; injected intradermally)
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)
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.
体外研究：
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。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 。
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.
体内研究：
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。Animal Model:Guinea pig (Injection of LTB4 10, 30, 100 ng/site; injected intradermally)
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)
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.
体外研究：
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。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 。
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