1610954-97-6
Chemical Structure
LX2761
- CAS No.: 1610954-97-6
- Formula:C32H47N3O6S
- Molecular Weight:601.80
IUPAC Name: 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
InChIKey: BNPZTRDIESRGTC-IXYVTWBDSA-N
SMILES: CC1=CC=C([C@H]2[C@H](O)[C@@H](O)[C@H](O)[C@@H](SC)O2)C=C1CC3=CC=C(CCCC(NC(C(NCCN(C)C)=O)(C)C)=O)C=C3
Biological Activity: LX2761 is an orally active, dual SGLT1/SGLT2 inhibitor with IC50 values of 2.2 nM and 2.7 nM against human SGLT1 and SGLT2, respectively. LX2761 locks human SGLT1 in an outward-open conformation and blocks its putative water permeation pathway. After oral administration, LX2761 is confined exclusively to the intestinal lumen, delays intestinal glucose absorption, regulates intestinal glucose metabolism, increases cecal glucose levels, reduces cecal pH, improves glycemic control and elevates plasma total GLP-1 levels. However, LX2761 induces diarrhea in a dose-dependent manner. LX2761 can be used in diabetes-related research[1][2][3].
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LX2761 | LX2761 is an orally active, dual SGLT1/SGLT2 inhibitor with IC50 values of 2.2 nM and 2.7 nM against human SGLT1 and SGLT2, respectively. LX2761 locks human SGLT1 in an outward-open conformation and blocks its putative water permeation pathway. After oral administration, LX2761 is confined exclusively to the intestinal lumen, delays intestinal glucose absorption, regulates intestinal glucose metabolism, increases cecal glucose levels, reduces cecal pH, improves glycemic control and elevates plasma total GLP-1 levels. However, LX2761 induces diarrhea in a dose-dependent manner. LX2761 can be used in diabetes-related research. | |||||||||||||||||||||
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- [1]. Spatola L, et al. SGLT1 and SGLT1 Inhibitors: A Role to Be Assessed in the Current Clinical Practice. Diabetes Ther. 2018;9(1):427-430. [Content Brief]
- [2]. Powell DR, et al. LX2761, a Sodium/Glucose Cotransporter 1 Inhibitor Restricted to the Intestine, Improves Glycemic Control in Mice. J Pharmacol Exp Ther. 2017;362(1):85-97. [Content Brief]
- [3]. Niu Y, et al. Structural mechanism of SGLT1 inhibitors. Nat Commun. 2022;13(1):6440. Published 2022 Oct 28. [Content Brief]
Keywords
