GSK-872 hydrochloride

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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。

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 mg

5 mg

10 mg

1 mM	2.3812 mL	11.9062 mL	23.8124 mL
5 mM	0.4762 mL	2.3812 mL	4.7625 mL
10 mM	0.2381 mL	1.1906 mL	2.3812 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。