1. GPCR/G Protein
  2. Leukotriene Receptor
  3. 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.

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CP-195543 Chemical Structure

CP-195543 Chemical Structure

CAS No. : 204981-48-6

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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].

IC50 & Target[1]

LTB4

 

In Vitro

CP-195543 inhibits human and mouse neu-trophil chemotaxis mediated by LTB4 with IC50 values of 2.4 nM, 7.5 nM, respectively[1].
CP-195543 (0.1 nM-10 µM; 60 min) blocks CD11b up-regulation on human neutrophils (HN) and murine neutrophils with IC50s of 270, 420 nM for human monocytes and eosinophils, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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) inhibits LTB4-mediated neutrophil infiltration in guinea pigskin in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

428.40

Formula

C24H19F3O4

CAS No.
SMILES

O=C(O)C1=CC=C(C(F)(F)F)C=C1C2=CC=C3[C@H](O)[C@@H](CC4=CC=CC=C4)COC3=C2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CP-195543
Cat. No.:
HY-112742
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