CP-195543

Modify Date: 2024-01-12 16:24:17

CP-195543 Structure
CP-195543 structure
Common Name CP-195543
CAS Number 204981-48-6 Molecular Weight 428.40000
Density N/A Boiling Point N/A
Molecular Formula C24H19F3O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name (3S,4R)-7-(2-carboxy-5-trifluoromethylphenyl)-4-hydroxy-3-benzyl-3,4-dihydro-2H-1-benzopyran
Synonym More Synonyms

 CP-195543 Biological Activity

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

[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.  

 Chemical & Physical Properties

Molecular Formula C24H19F3O4
Molecular Weight 428.40000
Exact Mass 428.12400
PSA 66.76000
LogP 5.35530

 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