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CP-96021 hydrochloride

Names

[ CAS No. ]:
167011-22-5

[ Name ]:
CP-96021 hydrochloride

Biological Activity

[Description]:

CP-96021 hydrochloride is a balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Ki values of 34 nM and 37 nM, respectively[1].

[Target]

LTC4:34 nM (Ki)

Platelet activating factor (PAF) receptor:37 nM (Ki)


[In Vivo]

In vivo, CP-96021 inhibits iv LTD4- and iv PAF-induced bronchoconstriction in guinea pigs with ED50s of 0.46 and 0.16 mg/kg p.o. respectively. CP-96021 effectively blocks the combined airway obstructive effects of endogenously released PAF and LTD4 stimulated by aerosolized antigen challenge in guinea pigs with an ED50s of 1.8 mg/kg p.o[1].

[References]

[1]. A. Marfat, et al. The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 1995, 5 (13): 1377-1382.

Chemical & Physical Properties

[ Molecular Formula ]:
C29H22ClFN4OS

[ Molecular Weight ]:
529.03

Related Compounds