0990CL 是能够与 Gαi 直接相互作用的，异源三聚体 Gαi subunit 特异性抑制剂。0990CL 能够阻断 α2AR 介导的 cAMP 调节。
货号:ajcx36670
CAS:511514-03-7
分子式:C21H21N5
分子量：343.42
溶解度:DMSO : 50 mg/mL (145.59 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP[1].

0990CL (100 nM-1 μM; 24 hours) is able to restore α2AR/Gαi mediated cAMP levels elicited by Fsk and UK14304 in HEK293 GloSensor cells. When the dosage is at 100 nM, it restores 31% of the reduction of cAMP[1].0990CL (30 μM; pre-treatment 30mins) shows selectivity for Gαi1 over Gαq. It demonstrates selectivity for Gαi and Gαq and results in a maximum endpoint fluorescence reduction of 38±8% and 10%, respectively[1].

[1]. Appleton KM,et al. Development of inhibitors of heterotrimeric Gαi subunits.Bioorg Med Chem. 2014 Jul 1;22(13):3423-34.