117690-79-6
中文名稱
1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE
英文名稱
1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE
CAS
117690-79-6
分子式
C19H28N4O3
分子量
360.45
MOL 文件
117690-79-6.mol
更新日期
2023/03/20 15:41:27
117690-79-6 結(jié)構(gòu)式
基本信息
中文別名
化合物LY 255283 英文別名
LY 255283CGS 23356
5'-Ethyl-2'-hydroxy-4'-[6-methyl-6-(1H-tetrazol-5-yl)heptyloxy]acetophenone
1-[5-ethyl-2-hydroxy-4-[6-methyl-6-(2H-tetrazol-5-yl)heptoxy]phenyl]ethanone
1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE
1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOLE-5-YL)HEPTYL]OXY]PHENYL]-ETHANONE
Ethanone, 1-[5-ethyl-2-hydroxy-4-[[6-methyl-6-(2H-tetrazol-5-yl)heptyl]oxy]phenyl]-
物理化學(xué)性質(zhì)
熔點160-162 °C
沸點573.4±60.0 °C(Predicted)
密度1.157±0.06 g/cm3(Predicted)
儲存條件Store at +4°C
溶解度二甲基亞砜：>20mg/mL
酸度系數(shù)(pKa)5.11±0.10(Predicted)
形態(tài)粉末
顏色灰白色至淡黃色
常見問題列表
生物活性
LY255283 是一種 leukotriene B4 (LTB4) receptor (BLT2) 的拮抗劑，可將 [3H]LTB4 從其在肺膜上的結(jié)合位點置換，pKi為7.0。靶點
| Target | Value |
|
BLT2
(Cell-free assay) | 7.0(pKi) |
體外研究
LY255283 competitively reduces conlractilc responses of lung parcnchyma to LTB, (pA
2
= 7.2).
LY255283 (10 μM, 7 days) significantly suppresses the invasiveness of highly aggressive 253 J-BV bladder cancer cells.
Cell Viability Assay
| Cell Line: | 253 J-BV cells. |
| Concentration: | 5 or 10 μM. |
| Incubation Time: | 7 days. |
| Result: | Inhibition of BLT2 signaling attenuates aggressive migration by 253 J-BV cells. |
體內(nèi)研究
LY255283 (3, 30 mg/kg) ameliorates lipopolysaccharide-induced ARDS in pigs, possibly by blocking the recruitment of activated PMNs into alveoli in a dose-dependent fashion.
LY255283 (2.5 mg/kg, ip) inhibits transitional cell carcinoma metastasis in mice models. The result suggests that a BLT2–Nox–ROS–NF–κB cascade plays a critical role in bladder cancer invasion and metastasis.
| Animal Model: | Mice (253 J-BV cells injected). |
| Dosage: | 2.5 mg/kg. |
| Administration: | IP injected 3 and 5 days after injection of cells. |
| Result: | By 12 weeks after injection, in mice treated with LY255283 only 0-3 nodules formed per lung, and histological analysis confirmed that the number of micrometastatic lesions was markedly reduced. |