128253-31-6

中文名称 BAY-X 1005

英文名称 (2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid

CAS 128253-31-6

分子式 C23H23NO3

分子量 361.43

MOL 文件 128253-31-6.mol

128253-31-6 结构式

基本信息物理化学性质安全数据常见问题列表

基本信息

英文别名

DG 031
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

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302

防范说明P280-P305+P351+P338

危险品标志Xn

危险类别码22

WGK Germany3

常见问题列表

生物活性

Veliflapon (BAY X 1005; DG-031) 是一种具有口服活性的，选择性的 5-脂氧合酶激活蛋白 (FLAP) 抑制剂。Veliflapon 也是白三烯 B4 和 C4 合成的抑制剂。

靶点

LTB ₄

LTC ₄

体外研究

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.

体内研究

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.