GSK-872|cas:1346546-69-7|西域试剂

GSK-872,99.86%

产品编号：Bellancom-101872| CAS NO：1346546-69-7| 分子式：C₁₉H₁₇N₃O₂S₂| 分子量：383.49

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-101872	￥860.00	杭州北京（现货）
Bellancom-101872	￥1450.00	杭州北京（现货）
Bellancom-101872	￥2700.00	杭州北京（现货）
Bellancom-101872	￥4900.00	杭州北京（现货）
Bellancom-101872	￥7800.00	杭州北京（现货）

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GSK-872

产品介绍

GSK-872 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 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 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.

体外研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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 (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 can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (260.76 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6076 mL	13.0381 mL	26.0763 mL
5 mM	0.5215 mL	2.6076 mL	5.2153 mL
10 mM	0.2608 mL	1.3038 mL	2.6076 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.52 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.52 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.42 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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