Abstract
The increasing number of people afflicted with diabetes throughout the world is a major health issue. Inhibitors of the sodium-dependent glucose cotransporters (SGLT) have appeared as viable therapeutics to control blood glucose levels in diabetic patents. Herein we report the discovery of LX2761, a locally acting SGLT1 inhibitor that is highly potent in vitro and delays intestinal glucose absorption in vivo to improve glycemic control.
MeSH terms
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Animals
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Benzhydryl Compounds / administration & dosage
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Benzhydryl Compounds / chemical synthesis
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Benzhydryl Compounds / chemistry
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Benzhydryl Compounds / pharmacology*
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Glucose / metabolism
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Glucose Tolerance Test
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Humans
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Hypoglycemic Agents / administration & dosage
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Hypoglycemic Agents / chemical synthesis
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Hypoglycemic Agents / chemistry
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Hypoglycemic Agents / pharmacology*
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Intestinal Absorption / drug effects
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Male
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Mice, Knockout
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Phenylbutyrates / administration & dosage
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Phenylbutyrates / chemical synthesis
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Phenylbutyrates / chemistry
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Phenylbutyrates / pharmacology*
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Sodium-Glucose Transporter 1 / antagonists & inhibitors*
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Structure-Activity Relationship
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Thioglycosides / administration & dosage
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Thioglycosides / chemical synthesis
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Thioglycosides / chemistry
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Thioglycosides / pharmacology*
Substances
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Benzhydryl Compounds
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Hypoglycemic Agents
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LX2761
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Phenylbutyrates
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SLC5A1 protein, human
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Slc5a1 protein, mouse
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Sodium-Glucose Transporter 1
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Thioglycosides
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Glucose