Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T54771 | ||||
Target Name | Sodium/glucose cotransporter 1 (SGLT1) | ||||
Type of Target |
Clinical trial |
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Drug Potency against Target | Drug Info | IC50 = 18700 nM | [1] | ||
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] | ||
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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