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GSK-872 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK-872 hydrochloride图片
CAS NO:2703752-81-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
GSK-872 hydrochloride 是RIPK3抑制剂,高亲和力结合 RIP3 激酶结构域,IC50为1.8 nM,并抑制激酶活性,IC50为1.3 nM。GSK-872 hydrochloride 降低 RIPK3 介导的坏死 (necroptosis) 和随后的 HMGB1 的细胞质易位和表达,并改善早期脑损伤中的脑水肿和神经功能缺损。
生物活性

GSK-872 hydrochloride is aRIPK3inhibitor, which binds RIP3 kinase domain with anIC50of 1.8 nM, and inhibits kinase activity with anIC50of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediatednecroptosisand subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury[1][2][3].

IC50& Target

IC50: 1.3 nM (RIPK3)[1]

体外研究
(In Vitro)

GSK-872 (GSK'872; 0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner[1].

Cell Viability Assay[1]

Cell Line:HT-29 cells
Concentration:0.01, 0.03 , 0.1, 0.3, 1, and 3 μM
Incubation Time:24 hours
Result:Blocked TNF-induced necroptosis in a concentration-dependent manner.
体内研究
(In Vivo)

GSK-872 hydrochloride (25 mM; intracerebroventricular injection) can attenuate brain edema and improve neurological function following subarachnoid hemorrhage (SAH) and reduce the number of necrotic cells. GSK-872 hydrochloride can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein[3].

Animal Model:Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model)[3]
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.
分子量

419.95

性状

Solid

Formula

C19H18ClN3O2S2

CAS 号

2703752-81-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 10 mg/mL(23.81 mM;ultrasonic and warming and heat to 60℃)

H2O : 2.5 mg/mL(5.95 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3812 mL11.9062 mL23.8124 mL
5 mM0.4762 mL2.3812 mL4.7625 mL
10 mM0.2381 mL1.1906 mL2.3812 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 0.21 mg/mL (0.50 mM); Clear solution

    此方案可获得 ≥ 0.21 mg/mL (0.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 2.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。