货号	规格	价格	上海	北京	珠海	重庆	武汉
S81535-1mg买3赠1	99.10%	￥229.00 S81535-1mg ￥229.00 现货（买3赠1）	9 9	-	-	-	-
S81535-5mg买3赠1	99.10%	￥526.00 S81535-5mg ￥526.00 现货（买3赠1）	6 6	-	-	-	-
S81535-10mg买3赠1	99.10%	￥722.00 S81535-10mg ￥722.00 现货（买3赠1）	6 6	-	-	-	-
S81535-25mg促销	99.10%	￥1530.00 ￥1220.00 S81535-25mg ￥1220.00 现货	5 5	-	-	-	-
S81535-50mg促销	99.10%	￥2700.00 ￥2160.00 S81535-50mg ￥2160.00 现货	4 4	-	-	-	-
S81535-100mg促销	≥98%	￥3800.00 ￥3040.00 S81535-100mg ￥3040.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM

靶点：

ROCK1:100 nM (IC50);GRK2:770 nM (IC50);ROCK; GRK; PKA

体外研究：

GSK180736A is a compound structurally similar to paroxetine that is developed as a ROCK inhibitor, is shown to be an even more potent and selective inhibitor of GRK2 with an IC50 of 0.77 μM and more than 100-fold selectivity over other GRKs. ROCK1 is a potential therapeutic target in the treatment of cardiovascular diseases such as hypertension. GSK180736A is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50=100 nM)

参考文献：

1. Waldschmidt HV, et al. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 28;59(8):3793-807.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.737 ml	13.685 ml	27.37 ml
5 mM	0.547 ml	2.737 ml	5.474 ml
10 mM	0.274 ml	1.369 ml	2.737 ml
50 mM	0.055 ml	0.274 ml	0.547 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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