LSN3318839 | GLP-1R PAM | Probechem Biochemicals

Chemical Structure : LSN3318839

LSN3318839 (LSN 3318839)

Catalog No.: PC-20512Not For Human Use, Lab Use Only.

LSN3318839 is a potent, positive allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R) with EC50 of 14 nM, Emax of 104%.

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Biological Activity

LSN3318839 is a potent, positive allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R) with EC50 of 14 nM, Emax of 104%.
LSN3318839 increases the potency and efficacy of the weak metabolite GLP-1(9-36)NH2 to become a full agonist at the GLP-1R and modestly potentiates the activity of the highly potent full-length ligand, GLP-1(7-36)NH2.
LSN3318839 preferentially enhances G protein-coupled signaling by the GLP-1R over β-arrestin recruitment.
LSN3318839 demonstrates robust glucose lowering in animal models alone or in treatment combination with sitagliptin.

Physicochemical Properties

M.Wt	480.39
Formula	C26H23Cl2N3O2
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	O=C(O)[C@H](C)C1=CC=CC=C1C2=CC3=C(N=CN3[C@@H](C4=C(Cl)C=CC(C5CC5)=C4Cl)C)C=N2

References

1. Francis S Willard, et al. J Med Chem. 2021 Mar 25;64(6):3439-3448.

LSN3318839 (LSN 3318839)

Biological Activity

Physicochemical Properties

References

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