产品
编 号：F425314
分子式：C30H30Cl2N6O2
分子量：577.5
分子式：C30H30Cl2N6O2
分子量：577.5
产品类型
规格
价格
是否有货
2mg
720
In-stock
5mg
1040
In-stock
10mg
1760
In-stock
25mg
3680
In-stock
结构图
CAS No: 6823-69-4
产品详情
生物活性：
GW4869 is a noncompetitive neutral sphingomyelinase (N-SMase) inhibitor with an IC50 of 1 μM. GW4869 is an inhibitor of exosome biogenesis/release.
体内研究：
GW4869 (2.5 μg/g，腹腔注射) 抑制小鼠的外泌体释放，从而阻断 LPS 刺激的促炎细胞因子产生和心脏炎症。GW4869 减轻 LPS 引起的心肌功能障碍并提高小鼠的存活率。 GW4869 (2.5 μg/g，ip) 阻断 CLP 小鼠促炎细胞因子的产生和心脏炎症。Animal Model:10-12 weeks old Male wild-type C57BL/6 mice (Endotoxin-Challenged Mice).
Dosage:2.5 μg/g.
Administration:I.P. once (1 h later, followed by an i.p. injection of LPS (2.5 μg/g, 100 μL)).
Result:Significantly decreased exosome levels by 37% in sera, compared to levels collected from control mice. At 12 h after LPS injection, the levels of circulating exosomeswere increased significantly compared to PBS-controls, as evidenced by a 1.7-fold elevation in the AChE activity.
Animal Model:10-12 weeks old Male wild-type C57BL/6 mice (CLP Polymicrobial Sepsis Model).
Dosage:2.5 μg/g.
Administration:I.P. once (before sham or CLP surgery).
Result:Decreased exosome concentration by 33% compared to mice injected with PBS in sham-surgery controls. CLP-stimulated exosome release was significantly inhibited by pre-treatment of CLP mice compared to CLP mice pre-treated with PBS.
体外研究：
GW4869 (10 μM) 部分抑制 TNF 诱导的鞘磷脂 (SM) 水解，20 μM 的化合物可完全防止 SM 损失。添加 10 -20 μM GW4869 可完全抑制神经酰胺的初始积累，而这种作用在稍后的时间点 (24 小时) 会部分消失。GW4869 的作用发生在谷胱甘肽下降的下游。GW4869 能够以剂量依赖性方式显著防止细胞死亡。 GW4869 (10 或 20 μM) 抑制外泌体释放和促炎细胞因子的产生巨噬细胞。GW4869 抑制神经酰胺介导的多泡体 (MVB) 向内出芽和从 MVB 释放成熟外泌体。 GW4869 还可以逆转 CCN2 3'-UTR 活性的抑制肝星状细胞中富含 miR-214 的外泌体。 溶解注意事项：GW4869 通常用 DMSO 配置悬浮液作为储备液，分装储存在 -80℃。
GW4869 is a noncompetitive neutral sphingomyelinase (N-SMase) inhibitor with an IC50 of 1 μM. GW4869 is an inhibitor of exosome biogenesis/release.
体内研究：
GW4869 (2.5 μg/g，腹腔注射) 抑制小鼠的外泌体释放，从而阻断 LPS 刺激的促炎细胞因子产生和心脏炎症。GW4869 减轻 LPS 引起的心肌功能障碍并提高小鼠的存活率。 GW4869 (2.5 μg/g，ip) 阻断 CLP 小鼠促炎细胞因子的产生和心脏炎症。Animal Model:10-12 weeks old Male wild-type C57BL/6 mice (Endotoxin-Challenged Mice).
Dosage:2.5 μg/g.
Administration:I.P. once (1 h later, followed by an i.p. injection of LPS (2.5 μg/g, 100 μL)).
Result:Significantly decreased exosome levels by 37% in sera, compared to levels collected from control mice. At 12 h after LPS injection, the levels of circulating exosomeswere increased significantly compared to PBS-controls, as evidenced by a 1.7-fold elevation in the AChE activity.
Animal Model:10-12 weeks old Male wild-type C57BL/6 mice (CLP Polymicrobial Sepsis Model).
Dosage:2.5 μg/g.
Administration:I.P. once (before sham or CLP surgery).
Result:Decreased exosome concentration by 33% compared to mice injected with PBS in sham-surgery controls. CLP-stimulated exosome release was significantly inhibited by pre-treatment of CLP mice compared to CLP mice pre-treated with PBS.
体外研究：
GW4869 (10 μM) 部分抑制 TNF 诱导的鞘磷脂 (SM) 水解，20 μM 的化合物可完全防止 SM 损失。添加 10 -20 μM GW4869 可完全抑制神经酰胺的初始积累，而这种作用在稍后的时间点 (24 小时) 会部分消失。GW4869 的作用发生在谷胱甘肽下降的下游。GW4869 能够以剂量依赖性方式显著防止细胞死亡。 GW4869 (10 或 20 μM) 抑制外泌体释放和促炎细胞因子的产生巨噬细胞。GW4869 抑制神经酰胺介导的多泡体 (MVB) 向内出芽和从 MVB 释放成熟外泌体。 GW4869 还可以逆转 CCN2 3'-UTR 活性的抑制肝星状细胞中富含 miR-214 的外泌体。 溶解注意事项：GW4869 通常用 DMSO 配置悬浮液作为储备液，分装储存在 -80℃。
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