LY-315920
|
|
|
- CAS号:
- 172733-42-5
- 英文名:
- NATRIUM[(1-BENZYL-2-ETHYL-3-OXAMOYLINDOOL-4-YL)OXY]ACETAAT
- 英文别名:
- LY 315920Na;LY 315920 sodium;Varespladib sodium;LY315920 sodiuM salt;VARESPLADIB SODIUM (LY315920 SODIUM SALT);NATRIUM[(1-BENZYL-2-ETHYL-3-OXAMOYLINDOOL-4-YL)OXY]ACETAAT;[[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid monosodium salt
- 中文名:
- LY-315920
- 中文别名:
- 伐瑞拉地钠;伐瑞拉迪钠
- CBNumber:
- CB01475683
- 分子式:
- C21H21N2NaO5
- 分子量:
- 404.4
- MOL File:
- 172733-42-5.mol
|
|
|
LY-315920化学性质
-
形态:
-
Solid
-
|
-
颜色:
-
Off-white to light yellow
-
|
LY-315920性质、用途与生产工艺
Varespladib sodium (LY315920 sodium) 是一种有效且具有选择性的 group IIA, secretory phospholipase A2 (sPLA2) 抑制剂，其 IC50 值为 9 nM。Varespladib sodium 对大鼠，兔，豚鼠和人等各种物种血清的 sPLA2 活性具有明显的抑制作用，IC50 分别为 8.1 nM，5.0 nM，3.2 nM 和 6.2 nM。
Varespladib sodium (10 μM; 24 and 48 hours; HCjE cells) treatment results in complete inhibition of the RA-induced increase in MUC16 protein detected in cell lysates at both time points.
Varespladib sodium (10 μM; 24 and 48 hours; HCjE cells) treatment significantly inhibits RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.
Western Blot Analysis
|
Cell Line:
|
HCjE cells
|
|
Concentration:
|
10 μM
|
|
Incubation Time:
|
24 hours, 48 hours
|
|
Result:
|
Significantly inhibited the RA-induced MUC16 protein expression at both time points.
|
RT-PCR
|
Cell Line:
|
HCjE cells
|
|
Concentration:
|
10 μM
|
|
Incubation Time:
|
24 hours, 48 hours
|
|
Result:
|
Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.
|
Varespladib sodium treatment inhibits human sPLA
2
-induced release of thromboxane A
2
(TXA
2
) from isolated guinea pig lung bronchoalveolar lavage cells with an
IC
50
of 0.79 μM. And the
ED
50
for Varespladib sodium is 16.1 mg/kg.
|
Animal Model:
|
Male Hartley guinea pigs (300-500 g)
|
|
Dosage:
|
3 mg/kg, 10 mg/kg, and 30 mg/kg
|
|
Administration:
|
Intravenous injection (Pharmacokinetic study)
|
|
Result:
|
Consistent inhibition of sPLA2 activity in BAL fluid was observed. Reduced the human sPLA2-induced generation of TXA2 on BAL cells from guinea pigs.
|
LY-315920
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-13402A | Varespladib sodium | | 1 mg | 750元 |
| 2024/08/19 | HY-13402A | Varespladib sodium | | 5 mg | 1650元 |
172733-42-5, LY-315920 相关搜索:
- C21H20N2O5Na
- 伐瑞拉地钠
- 伐瑞拉迪钠
- 172733-42-5
- VARESPLADIB SODIUM (LY315920 SODIUM SALT)
- Varespladib sodium
- LY 315920Na
- LY 315920 sodium
- [[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid monosodium salt
- LY315920 sodiuM salt
- NATRIUM[(1-BENZYL-2-ETHYL-3-OXAMOYLINDOOL-4-YL)OXY]ACETAAT