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172733-42-5

中文名稱(chēng) LY-315920
英文名稱(chēng) NATRIUM[(1-BENZYL-2-ETHYL-3-OXAMOYLINDOOL-4-YL)OXY]ACETAAT
CAS 172733-42-5
分子式 C21H19N2NaO5
分子量 402.376
MOL 文件 172733-42-5.mol
172733-42-5 結(jié)構(gòu)式 172733-42-5 結(jié)構(gòu)式

基本信息

中文別名
伐瑞拉迪鈉
英文別名
LY 315920Na
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

物理化學(xué)性質(zhì)

形態(tài)Solid
顏色Off-white to light yellow
LY-315920價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2025/02/08HY-13402AVarespladib sodium172733-42-51 mg750元
2025/02/08HY-13402ALY-315920
Varespladib sodium
172733-42-510 mM * 1 mLin DMSO1461元
2025/02/08HY-13402AVarespladib sodium172733-42-55 mg1650元

常見(jiàn)問(wèn)題列表

生物活性
Varespladib sodium (LY315920 sodium) 是一種有效且具有選擇性的 group IIA, secretory phospholipase A2 (sPLA2) 抑制劑,其 IC50 值為 9 nM。Varespladib sodium 對(duì)大鼠,兔,豚鼠和人等各種物種血清的 sPLA2 活性具有明顯的抑制作用,IC50 分別為 8.1 nM,5.0 nM,3.2 nM 和 6.2 nM。
靶點(diǎn)

sPLA2

9 nM (IC 50 )

體外研究

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.
體內(nèi)研究

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.
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