货号	规格	价格	上海	北京	珠海	重庆	武汉
S84038-1mg买3赠1	98.50%	￥460.00 S84038-1mg ￥460.00 现货（买3赠1）	9 9	-	-	-	-
S84038-5mg促销	98.50%	￥1150.00 ￥920.00 S84038-5mg ￥920.00 现货	6 6	-	-	-	-
S84038-10mg促销	98.50%	￥1900.00 ￥1520.00 S84038-10mg ￥1520.00 现货	4 4	-	-	-	-

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产品描述：

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.

靶点：

IC50 & Target: 3.9±1.0 μM (GRK1), 0.15±0.07 μM (GRK2), 0.38±0.06 μM (GRK5), 120±40 μM (PKA);GRK; PKA

体外研究：

CCG215022 has nanomolar potency against both GRK2 and GRK5 and is at least 20-fold more potent than Paroxetine. In the course of a GRK2 structure-based drug design campaign, CCG215022 exhibits nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA. Treatment of murine cardiomyocytes with CCG215022 results in significantly increases contractility at 20-fold lower concentrations than Paroxetine, an inhibitor with more modest selectivity for GRK2

参考文献：

1. Homan KT, et al. Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally DesignedInhibitor. J Biol Chem. 2015 Aug 21;290(34):20649-59.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.002 ml	10.01 ml	20.02 ml
5 mM	0.4 ml	2.002 ml	4.004 ml
10 mM	0.2 ml	1.001 ml	2.002 ml
50 mM	0.04 ml	0.2 ml	0.4 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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