| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T22583 | ||||
| Target Name | Sodium/glucose cotransporter 2 | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | Dapagliflozin | Drug Info | EC50 = 1.12 nM/L | [552801] | |
| Action against Disease Model | Dapagliflozin | Dapagliflozin potently and selectively inhibited h uMan SGLT2 versus h uMan SGLT1, the major cotransporter of glucose in the gut, and did not significantly inhibit facilitative glucose transport in h uMan adipocytes. In vivo, dapagliflozin acutely induced renal glucose excretion in normal and diabetic rats, improved glucose tolerance in normal rats, and reduced hyperglycemiain Zucker diabetic fatty (ZDF) rats after single oral doses ranging from 0.1 to 1.0 mg/kg. | [552801] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | The L. mexicana genome encodes three related glucose transporter genes, designated LmGT1, LmGT2,and LmGT3.A knockout of this gene cluster, generated by homologous gene replacement, was unable to replicate as amastigotes(the mammalian life-cycle stage) inside murine macrophages,to survive as the culture form of amastigotes, or to induce lesions in BALB/c mice (R. Burchmore and G. Coombs, personal communication) | [552801] | |||
| References | |||||
| Ref 552801 | Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes. 2008 Jun;57(6):1723-9. doi: 10.2337/db07-1472. Epub 2008 Mar 20. | ||||
| Ref 552801 | Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes. 2008 Jun;57(6):1723-9. doi: 10.2337/db07-1472. Epub 2008 Mar 20. | ||||
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