产品
编 号：F129018
分子式：C19H17N3O2S2
分子量：383.49
分子式：C19H17N3O2S2
分子量：383.49
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
946
In-stock
1mg
342
In-stock
5mg
860
In-stock
10mg
1450
In-stock
25mg
2700
In-stock
50mg
3780
In-stock
100mg
5295
In-stock
结构图
CAS No: 1346546-69-7
产品详情
生物活性：
GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
体内研究：
GSK-872 (25 mM；脑室内注射) 可减轻蛛网膜下腔出血 (SAH) 后的脑水肿并改善神经功能，并减少坏死细胞的数量。GSK-872 还可以降低 RIPK3 和 MLKL 的蛋白水平，以及 HMGB1 的细胞质易位和表达，HMGB1 是一种重要的促炎蛋白。Animal Model:Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model)
Dosage:25 mM/6 μL
Administration:Syringe pump (intracerebroventricular) at 30 min after SAH
Result:Attenuated brain edema, improved neurological function and decreased the number of necrotic cells in the ipsilateral cortex. Decreased the expression of RIPK3, MLKL and cytoplasmic HMGB1 at 72 h after SAH in the ipsilateral cortex.
体外研究：
GSK-872 (GSK'872；0.01-3 μM；24 小时) 以浓度依赖性方式阻断 TNF 诱导的人 HT-29 细胞坏死性凋亡。
GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
体内研究：
GSK-872 (25 mM；脑室内注射) 可减轻蛛网膜下腔出血 (SAH) 后的脑水肿并改善神经功能，并减少坏死细胞的数量。GSK-872 还可以降低 RIPK3 和 MLKL 的蛋白水平，以及 HMGB1 的细胞质易位和表达，HMGB1 是一种重要的促炎蛋白。Animal Model:Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model)
Dosage:25 mM/6 μL
Administration:Syringe pump (intracerebroventricular) at 30 min after SAH
Result:Attenuated brain edema, improved neurological function and decreased the number of necrotic cells in the ipsilateral cortex. Decreased the expression of RIPK3, MLKL and cytoplasmic HMGB1 at 72 h after SAH in the ipsilateral cortex.
体外研究：
GSK-872 (GSK'872；0.01-3 μM；24 小时) 以浓度依赖性方式阻断 TNF 诱导的人 HT-29 细胞坏死性凋亡。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备