产品
编 号：F618023
分子式：C19H18ClN3O2S2
分子量：419.95
分子式：C19H18ClN3O2S2
分子量：419.95
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 2703752-81-0
产品详情
生物活性：
GSK-872 hydrochloride 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 hydrochloride 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 hydrochloride (25 mM；intracerebroventricuLar injection) 可以减轻蛛网膜下腔出血 (SAH) 后的脑水肿和改善神经功能，并减少坏死细胞的数量。GSK-872 hydrochloride 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 hydrochloride (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 hydrochloride 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 hydrochloride 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 hydrochloride (25 mM；intracerebroventricuLar injection) 可以减轻蛛网膜下腔出血 (SAH) 后的脑水肿和改善神经功能，并减少坏死细胞的数量。GSK-872 hydrochloride 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 hydrochloride (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。
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