128253-31-6
128253-31-6 結(jié)構(gòu)式
基本信息
BAY 1005
Velifapon
BAY-X 1005
VELIFLAPON
BAY-X-1005 >=98% (HPLC)
ZEYYDOLCHFETHQ-JOCHJYFZSA-N
2-(4-(quinolin-2-yl-methoxy)phenyl)-2-cyclopentylacetic acid
α-Cyclopentyl-4-(2-quinolinylmethoxy)-(R)-benzeneacetic acid
(αR)-α-Cyclopentyl-4-(2-quinolinylmethoxy)-benzeneacetic acid
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見(jiàn)問(wèn)題列表
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LTB 4
|
LTC 4
|
Veliflapon (BAY X 1005; DG-031) effectively inhibits the synthesis of LTB4 in A23187-stimulated leukocytes from rats, mice and humans (IC
50
s of 0.026, 0.039 and 0.22 μM, respectively) as well as the formation of LTC4 (IC
50
of 0.021 μM) in mouse peritoneal macrophages stimulated with opsonized zymosan.
Veliflapon (BAY X 1005; DG-031; diet; 18.8 mg/kg/day for 16 weeks ) inhibits atherogenesis.
Veliflapon after topical (18 μg/ear) and oral (48.7 mg/kg) administration has antiedematous effects in the arachidonic acid-induced mouse ear inflammation test.
Veliflapon is potent (11.8 and 6.7 mg/kg p.o. at 1 and 5 hours, respectively) and has a long duration of action (ED
40
of 16 hours, 70 mg/kg p.o.) in the rat whole blood ex vivo leukotriene B4 inhibition assay.
| Animal Model: | Female apoE/LDLR-DKO mouse model |
| Dosage: | 18.8 mg/kg |
| Administration: | Diet; per day during 16 weeks |
| Result: | Inhibited atherogenesis. |