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AS408

Chemical Structure : AS408

CAS No.: 2378521-26-5

AS408 (AS-408)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 315.174
Formula C14H11BrN4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-bromo-N2-phenylquinazoline-2,4-diamine

References

1. Liu X, et al. Nat Chem Biol. 2020 Jul;16(7):749-755.

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