| Description | 0990CL is an effective heterotrimer Gαi subunit specific inhibitor, which can interact with purified Go± in GDP-bound state, and can block α2AR mediated cAMP regulation. In the cell model, low concentration of 0990CL could partially restore cAMP level, and high concentration of 0990CL (10μM) began to have negative effects on cell viability. |
| In vitro | 0990CL（以30 μM浓度预处理30分钟）展现出对Gαi1的优先结合能力，相较于Gαq。它对Gαi和Gαq显示出选择性，导致终点荧光的最大降低分别为38±8%和10%。使用0990CL处理（100 nM至1 μM，24小时）能够在HEK293 GloSensor细胞中恢复由Fsk和UK14304诱导的α2AR/Gαi介导的cAMP水平。在100 nM剂量下，它能够恢复31%的降低的cAMP水平[1]。 |
| molecular weight | 343.42 |
| Molecular formula | C21H21N5 |
| CAS | 511514-03-7 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45.0 mg/mL (131.0 mM), Sonication is recommended. |
| References | 1. Appleton KM,et al. Development of inhibitors of heterotrimeric Gαi subunits.Bioorg Med Chem. 2014 Jul 1;22(13):3423-3434. |