| Bioactivity | 0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP[1]. | ||||||||||||
| Target | IC50: Gαi subunit | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | 0990CL | ||||||||||||
| CAS | 511514-03-7 | ||||||||||||
| Formula | C21H21N5 | ||||||||||||
| Molar Mass | 343.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Appleton KM,et al. Development of inhibitors of heterotrimeric Gαi subunits.Bioorg Med Chem. 2014 Jul 1;22(13):3423-34. |