Target Validation Information
TTD ID T54771
Target Name Sodium/glucose cotransporter 1 (SGLT1)
Type of Target
Clinical trial
Drug Potency against Target KURARINONE Drug Info IC50 = 10400 nM [1]
O-spiroketal glucoside Drug Info IC50 = 1300 nM [3]
QCP Drug Info IC50 = 2.1 nM [2]
QSPac Drug Info IC50 = 0.17 nM [2]
Sophoraflavanone G Drug Info IC50 = 18700 nM [1]
Action against Disease Model Phlorizin Drug Info The phlorizin binding properties of l uMinal membrane vesicles isolated from the LLC-PK1 cells, a continuous epithelial cell line derived from pig kidney, are studied. Scatchardanalysis of this binding indicates the existence of a single high affinity sodi uM-dependent site with KD = 0.4 microM at 266 mM sodi uM. [4]
References
REF 1 Na+-glucose cotransporter (SGLT) inhibitory flavonoids from the roots of Sophora flavescens. Bioorg Med Chem. 2007 May 15;15(10):3445-9.
REF 2 Tripeptides of RS1 (RSC1A1) inhibit a monosaccharide-dependent exocytotic pathway of Na+-D-glucose cotransporter SGLT1 with high affinity. J Biol Chem. 2007 Sep 28;282(39):28501-13.
REF 3 ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors. Bioorg Med Chem. 2010 Jun 15;18(12):4422-32.
REF 4 J Biol Chem. 1988 Jan 5;263(1):187-92.High affinity phlorizin binding to the LLC-PK1 cells exhibits a sodium:phlorizin stoichiometry of 2:1.

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