172733-42-5
基本信息
LY 315920 sodium
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
物理化学性质
| 形态 | Solid |
| 颜色 | Off-white to light yellow |
常见问题列表
|
sPLA2 9 nM (IC 50 ) |
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. |