Arrestin Antagonist
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ML339
0 ImagesML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research.
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D1R antagonist 2
0 ImagesCat. No.: HY-178103D1R antagonist 2 (Compound 13a) is a BBB-penetrable D1R antagonist with IC50s of 35.6 and 70 nM for cAMP-based D1R and β-arrestin-based D1R, respectively. D1R antagonist 2 effectively antagonizes D1R-mediated cAMP and β-arrestin recruitment. D1R antagonist 2 can be used for neurodegenerative and neuropsychiatric diseases such as schizophrenia, Parkinson’s disease and Alzheimer’s disease research.
