Chemical Structure : AS408
货号: PC-49058Not For Human Use, Lab Use Only.
AS408 is a negative allosteric modulator of the β2-adrenergic receptor (β2AR) for both G-protein activation and arrestin recruitment (pKB=6.8, [35S]GTPγS binding assays), binds to a pocket formed by the membrane-facing surface of TM3 and TM5.
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AS408 is a negative allosteric modulator of the β2-adrenergic receptor (β2AR) for both G-protein activation and arrestin recruitment (pKB=6.8, [35S]GTPγS binding assays), binds to a pocket formed by the membrane-facing surface of TM3 and TM5.
AS408 exhibits negative allosteric regulation of norepinephrine-stimulated arrestin recruitment and cAMP accumulation.
AS408 can stabilize TM5 in an inactive conformation does not bind to the G protein-stabilized active state of the β2AR.
分子量 | 315.174 | |
分子式 | C14H11BrN4 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Liu X, et al. Nat Chem Biol. 2020 Jul;16(7):749-755.
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