BAY-X 1005
| 中文名称 | BAY-X 1005 |
|---|---|
| 中文同义词 | 化合物 T13295;化合物 VELIFLAPON |
| 英文名称 | (2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid |
| 英文同义词 | (2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid;2-(4-(quinolin-2-yl-methoxy)phenyl)-2-cyclopentylacetic acid;BAY-X 1005;BAY 1005;DG 031;Velifapon;(αR)-α-Cyclopentyl-4-(2-quinolinylmethoxy)-benzeneacetic acid;α-Cyclopentyl-4-(2-quinolinylmethoxy)-(R)-benzeneacetic acid |
| CAS号 | 128253-31-6 |
| 分子式 | C23H23NO3 |
| 分子量 | 361.43 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 128253-31-6.mol |
| 结构式 |  |
BAY-X 1005 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） |
| 形态 | 粉末 |
| 酸度系数(pKa) | 4.47±0.10(Predicted) |
| 颜色 | 白色至米色 |
| InChI | 1S/C23H23NO3/c25-23(26)22(17-6-1-2-7-17)18-10-13-20(14-11-18)27-15-19-12-9-16-5-3-4-8-21(16)24-19/h3-5,8-14,17,22H,1-2,6-7,15H2,(H,25,26)/t22-/m1/s1 |
| InChIKey | ZEYYDOLCHFETHQ-JOCHJYFZSA-N |
| SMILES | OC(=O)[C@H](C1CCCC1)c2ccc(OCc3ccc4ccccc4n3)cc2 |
|
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. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/09/15 | HY-14165 | BAY-X 1005 Veliflapon | 128253-31-6 | 5mg | 2500元 |
| 2026/09/15 | HY-14165 | Veliflapon | 128253-31-6 | 10 mM * 1 mLin DMSO | 2750元 |