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Volumn 13, Issue 6, 2003, Pages 1067-1070

The identification of clinical candidate SB-480848: A potent inhibitor of lipoprotein-associated phospholipase A2

Author keywords

[No Author keywords available]

Indexed keywords

BIPHENYL DERIVATIVE; DARAPLADIB; FUNCTIONAL GROUP; PHOSPHOLIPASE A2; PHOSPHOLIPASE A2 INHIBITOR; PYRIMIDINONE DERIVATIVE; RECOMBINANT PROTEIN; SB 435495; UNCLASSIFIED DRUG;

EID: 0037463766     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00058-1     Document Type: Article
Times cited : (120)

References (12)
  • 9
    • 84992229008 scopus 로고    scopus 로고
    • note
    • Oral bioavailability was determined for the free base of 21 as described in ref 5, except that the iv infusion was in normal saline containing 10% (w/v) Encapsin and 2% (v/v) DMSO and the oral dose by gavage administration in 1% aq methylcellulose (rat) or by loose filled gelatine capsule (dog). The fed:fasted ratio in the rat was measured by oral gavage administration (10 mg/kg in 1% Tween 80 and 1% aq methylcellulose) to the conscious, cannulated fed or fasted male rat. Serial blood samples were collected up to 14 h post dose and analysed by LC/MS/MS. The fed:fasted ratio was calculated as AUC (fed)/AUC (fasted).
  • 10
    • 84992264993 scopus 로고    scopus 로고
    • note
    • 2S requires 666.
  • 12
    • 84992251231 scopus 로고    scopus 로고
    • note
    • Determined as in ref 5, data from 15 month old female WHHL rabbits. Compound 1 gave an inhibition of 74±9% in sex and age (14 months) matched WHHL rabbits.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.