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Ki = 2 nM

galacto-Dapagliflozin is a potent inhibitor of human SGLT2.

Renal glucose transport is mediated by sodium-glucose cotransporters (SGLT) 1 and 2. In humans, SGLT2 is responsible for the majority of glucose reabsorption in the kidney.

In vitro: It was found that galacto-dapagliflozin was a selective inhibitor of hSGLT2, but was less potent than dapagliflozin for both transporters. Both phlorizin and galacto-dapagliflozin rapidly dissociated from SGLT2, while dapagliflozin and fluoro-dapagliflozin dissociated from hSGLT2 at a rate 10-fold slower. Dapagliflozin, fluoro-dapagliflozin, and galacto-dapagliflozin dissociated quickly from hSGLT1, and phlorizin readily exchanged with dapagliflozin bound to hSGLT1 [1].

In vivo: Male db/db mice were administered dapagliflozin for 12 weeks. Results showed that administration of dapagliflozin could ameliorate hyperglycemia, β-cell damage and albuminuria in db/db mice. Serum creatinine, creatinine clearance and blood pressure were not affected by administration of dapagliflozin. Dapagliflozin treatment was able to decrease macrophage infiltration in the kidney of db/db mice [2].

Clinical trial: Previous clinical study found that lowering the plasma glucose concentration with dapagliflozin could markedly improve β-cell function, which provided strong support for the glucotoxic effect of hyperglycemia on β-cell function [3].

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