GSK854

Name: GSK854
Brand: TargetMol
SKU: T24115
Price: 997 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 98.91%

货号 T24115Cas号 1316059-00-3

别名 GSK-854, GSK 854

GSK854 是一种具有高选择性和有效性的肌钙蛋白 I 相互作用激酶 (TNNI3K) 抑制剂，抑制小鼠心肌梗死损伤细胞焦亡和细胞凋亡，可限制缺血性心脏的氧化应激、损伤和不良重塑。

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GSK854

一键复制产品信息

很棒

纯度: 98.91%

货号 T24115 别名 GSK-854, GSK 854Cas号 1316059-00-3

规格	价格	库存
1 mg	¥ 997	现货
5 mg	¥ 2,480	现货
10 mg	¥ 3,980	现货
25 mg	¥ 6,270	现货
50 mg	¥ 8,460	现货
100 mg	¥ 11,300	现货
200 mg	¥ 15,300	现货
1 mL x 10 mM (in DMSO)	¥ 2,630	现货

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纯度: 98.91%

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资源下载:

COA LCMS HNMR 产品操作手册

产品介绍

GSK854 AI Summary

GSK854 exhibits potent bioactivity in inhibiting TNNI3K, with an IC50 value of <= 10.0 nM for binding to human full-length TNNI3K and an IC50 of 8.0 nM for inhibiting TNNI3K autophosphorylation. It demonstrates high selectivity against BRAF, with an IC50 of 250.0 nM, and a selectivity index ratio of at least 25.0. The compound shows promising oral bioavailability in rat plasma at 48.0%, a moderate volume of distribution at steady state of 1.9 L/kg, and a relatively short half-life of 2.3 hours. Furthermore, notable drug uptake is observed in various tissues in mice, with concentrations of 0.4 μM in blood and 1.1 μM in the heart, indicating its potential therapeutic applications targeting TNNI3K..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	GSK854 is a highly selective and potent inhibitor of troponin I interacting kinase (TNNI3K) that inhibits myocardial infarction-injured cellular pyroptosis and apoptosis in mice, which may limit oxidative stress, injury, and adverse remodeling in the ischemic heart.
别名	GSK-854, GSK 854

化学信息

分子量	482.96
分子式	C₁₈H₁₉ClN₆O₄S₂
CAS No.	1316059-00-3
Smiles	CCS(=O)(=O)c1ccc(cc1Nc1cc(Nc2ccc(Cl)cn2)ncn1)S(=O)(=O)NC
密度	1.31g/cm3
颜色	White
物理性状	Solid

储存&溶解度

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 100 mg/mL (207.06 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.28 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0706 mL	10.3528 mL	20.7056 mL	103.5282 mL
5 mM	0.4141 mL	2.0706 mL	4.1411 mL	20.7056 mL
10 mM	0.2071 mL	1.0353 mL	2.0706 mL	10.3528 mL
20 mM	0.1035 mL	0.5176 mL	1.0353 mL	5.1764 mL
50 mM	0.0414 mL	0.2071 mL	0.4141 mL	2.0706 mL
100 mM	0.0207 mL	0.1035 mL	0.2071 mL	1.0353 mL