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LX2761

Chemical Structure : LX2761

CAS No.: 1610954-97-6

LX2761 (LX 2761;LX-2761)

Catalog No.: PC-60689Not For Human Use, Lab Use Only.

A potent, locally acting and orally bioavailable SGLT1 inhibitor that inhibits human SGLT1- and SGLT2-mediated glucose uptake with IC50 of 2.2 nM and 2.7 nM, respectively, restricted to the intestinal lumen.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, locally acting and orally bioavailable SGLT1 inhibitor that inhibits human SGLT1- and SGLT2-mediated glucose uptake with IC50 of 2.2 nM and 2.7 nM, respectively, restricted to the intestinal lumen; synergistically increases active GLP-1 levels combined with sitagliptin, lowers postprandial glucose, fasting glucose, and hemoglobin A1C, and increased plasma total GLP-1 in mice; delays intestinal glucose absorption in vivo to improve glycemic control.

Diabetes

Phase 1 Clinical

Physicochemical Properties

M.Wt 601.803
Formula C32H47N3O6S
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

N-(1-((2-(Dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2H-pyran-2-yl)benzyl)phenyl)-butanamide

References

1. Goodwin NC, et al. J Med Chem. 2017 Jan 26;60(2):710-721.

2. Powell DR, et al. J Pharmacol Exp Ther. 2017 Jul;362(1):85-97.

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