204981-48-6
204981-48-6 structure
- Name: CP-195543
- Chemical Name: (3S,4R)-7-(2-carboxy-5-trifluoromethylphenyl)-4-hydroxy-3-benzyl-3,4-dihydro-2H-1-benzopyran
- CAS Number: 204981-48-6
- Molecular Formula: C24H19F3O4
- Molecular Weight: 428.40000
- Catalog: Signaling Pathways GPCR/G Protein Leukotriene Receptor
- Create Date: 2016-09-12 16:53:05
- Modify Date: 2025-08-25 17:45:34
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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].
| Name | (3S,4R)-7-(2-carboxy-5-trifluoromethylphenyl)-4-hydroxy-3-benzyl-3,4-dihydro-2H-1-benzopyran |
|---|---|
| Synonyms |
2-[(3S,4R)-3,4-dihydro-4-hydroxy-3-(phenylmethyl)-2H-1-benzopyran-7-yl]-4-(trifluoromethyl)benzoic acid
(3S-trans)-2-[3,4-dihydro-4-hydroxy-3-(phenylmethyl)-2H-1-benzopyran-7-yl]-4-(trifluoromethyl)-benzoic acid |
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
LTB4 |
| In Vitro | 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]。 |
| In Vivo | 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. |
| References |
| Molecular Formula | C24H19F3O4 |
|---|---|
| Molecular Weight | 428.40000 |
| Exact Mass | 428.12400 |
| PSA | 66.76000 |
| LogP | 5.35530 |