LY-315920
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- CAS號:
- 172733-42-5
- 英文名:
- NATRIUM[(1-BENZYL-2-ETHYL-3-OXAMOYLINDOOL-4-YL)OXY]ACETAAT
- 英文別名:
- 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
- 中文別名:
- 伐瑞拉地鈉;伐瑞拉迪鈉
- CBNumber:
- CB01475683
- 分子式:
- C21H21N2NaO5
- 分子量:
- 404.4
- MOL File:
- 172733-42-5.mol
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LY-315920化學(xué)性質(zhì)
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形態(tài):
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Solid
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顏色:
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Off-white to light yellow
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LY-315920性質(zhì)、用途與生產(chǎn)工藝
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。
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
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Cell Line:
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HCjE cells
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Concentration:
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10 μM
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Incubation Time:
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24 hours, 48 hours
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Result:
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Significantly inhibited the RA-induced MUC16 protein expression at both time points.
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RT-PCR
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Cell Line:
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HCjE cells
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Concentration:
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10 μM
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Incubation Time:
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24 hours, 48 hours
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Result:
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Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.
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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.
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Animal Model:
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Male Hartley guinea pigs (300-500 g)
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Dosage:
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3 mg/kg, 10 mg/kg, and 30 mg/kg
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Administration:
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Intravenous injection (Pharmacokinetic study)
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Result:
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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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LY-315920
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS編號 | 包裝 | 價(jià)格 |
|---|
| 2025/02/08 | HY-13402A | Varespladib sodium | 172733-42-5 | 1 mg | 750元 |
| 2025/02/08 | HY-13402A | LY-315920
Varespladib sodium | 172733-42-5 | 10 mM * 1 mLin DMSO | 1461元 |
172733-42-5, LY-315920 相關(guān)搜索:
- 抑制劑
- C21H20N2O5Na
- 伐瑞拉地鈉
- 伐瑞拉迪鈉
- 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