A GPR75 antagonist
货号:ajcx24140
CAS:N/A
分子式:C24H39NO6•2Na
分子量：483.5
溶解度:DMSO: slightly soluble,PBS (pH 7.2): 1 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

AAA is an antagonist of G protein-coupled receptor 75 (GPR75).¹It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 µM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.²

1.CÁrdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.SedlÁkovÁ, L., KikerlovÁ, S., HuskovÁ, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)