规格

价格

库存

数量

1 mg

¥ 253

现货

2 mg

¥ 358

现货

5 mg

¥ 589

现货

10 mg

¥ 849

现货

25 mg

¥ 1,670

现货

50 mg

¥ 2,970

现货

100 mg

¥ 3,820

现货

500 mg

¥ 8,450

现货

1 mL x 10 mM (in DMSO)

¥ 497

现货

生物活性

产品描述	GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).
靶点活性	ROCK1:100 nM, GRK2:0.77 μM
体外活性	GSK180736A 对 GRK2 表现出 770 nM 的 IC50 值，并且对 GRK5 的抑制效力低 300 倍[2]。它对 PKA 是弱抑制剂，IC50 为 30 μM，但对 ROCK1 具有高度的抑制效果（IC50 = 100 nM）[3]。
细胞实验	Cardiac myocytes are isolated from LV free wall and septum of C57/Bl6 mice. Cells are treated with isoproterenol (0.5 μM) for 2 min for the recording of contraction, with pretreatment of either PBS as vehicle or paroxetine (10 μM), 215022 (0.1, 0.5, 1, 10 μM), 215023 (0.1, 0.5, 1, 10 μM), 224064 (0.1, 0.5, 1, 10 μM), and GSK180736A ( 0.5, 1 μM), for 10 min[1].
别名	GSK180736

化学信息

分子量	365.36
分子式	C₁₉H₁₆FN₅O₂
CAS No.	817194-38-0
Smiles	CC1=C(C(NC(=O)N1)c1ccc(F)cc1)C(=O)Nc1ccc2[nH]ncc2c1
密度	no data available

储存&溶解度

存储

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

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 60 mg/mL (164.22 mM), Sonication is recommended.

Ethanol: 3 mg/mL (8.21 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.47 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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7370 mL	13.6851 mL	27.3703 mL	136.8513 mL
5 mM	0.5474 mL	2.7370 mL	5.4741 mL	27.3703 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.2737 mL	1.3685 mL	2.7370 mL	13.6851 mL
20 mM	0.1369 mL	0.6843 mL	1.3685 mL	6.8426 mL
50 mM	0.0547 mL	0.2737 mL	0.5474 mL	2.7370 mL
100 mM	0.0274 mL	0.1369 mL	0.2737 mL	1.3685 mL