128253-31-6
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
物理化学性质
| 熔点 | 169-171 °C |
| 沸点 | 555.4±40.0 °C(Predicted) |
| 密度 | 1.242±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO：可溶，5mg/mL（澄清溶液） |
| 酸度系数(pKa) | 4.47±0.10(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
常见问题列表
|
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. |