CCG258208 hydrochloride (Synonyms: GRK2-IN-1 hydrochloride)
目录号: PL01799 纯度: ≥98%
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PL01799-1mg 1mg ¥1483.64 请登录
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PL01799-10mM*1mLinDMSO 10mM*1mLinDMSO ¥4654.91 请登录
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中文名称
CCG258208 hydrochloride
英文名称
CCG258208 hydrochloride
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
CCG258208 (GRK2-IN-1) hydrochloride 是一种强效和选择性的 GRK2 (G蛋白偶联受体激酶2) 抑制剂 (IC50=30 nM),对 GRK5 (IC50=7.09 μM) 显示出 230 倍的选择性,对 GRK1 (IC50=87.3 μM)、PKA 和 ROCK1 有超过 2500 倍的选择性。CCG258208 hydrochloride 可用于心衰的研究。
生物活性
CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC 50 =30 nM) while maintaining 230-fold selectivity over GRK5 (IC 50 =7.09 μM) and more than 2500-fold selectivity over GRK1 (IC 50 =87.3 μM), PKA, and ROCK1. CCG258208 hydrochloride can be used in heart failure research.
性状
Solid
IC50 & Target[1][2]
GRK2 30 nM (IC50) GRK5 7.1 μM (IC50
体外研究(In Vitro)
CCG258208 (Compound 14as) (0-1 μM; 10 min) shows significant improvement in βAR-stimulated contractility in mouse cardiomyocytes. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
CCG258208 (Compound 14as) (intraperitoneal injection; 10 mg/kg; once) treatment shows superior half-life in vivo. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CD-1 mice
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069.
溶解度数据
In Vitro: DMSO : 250 mg/mL (511.31 mM; Need ultrasonic)H2O : 50 mg/mL (102.26 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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