galacto-Dapagliflozin

- Overview
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    Background
    
    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].
    
    [1] Hummel, C. S.,Lu, C.,Liu, J., et al. Structural selectivity of human SGLT inhibitors. American Journal of Physiology.Cell Physiology 302(2), C373-C382 (2012).
    [2] Terami N et al. Long-term treatment with the sodium glucose cotransporter 2 inhibitor, dapagliflozin, ameliorates glucose homeostasis and diabetic nephropathy in db/db mice. PLoS One. 2014 Jun 24;9(6):e100777.
    [3] Merovci A et al. Dapagliflozin lowers plasma glucose concentration and improves β-cell function. J Clin Endocrinol Metab. 2015 May;100(5):1927-32.
- Properties
  - Alternative Name
    
    (1S)-1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-D-galactitol
    
    CAS Number
    
    1408245-02-2
    
    Molecular Formula
    
    C21H25ClO6
    
    Molecular Weight
    
    408.9
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥ 95.00%
    
    Solubility
    
    ≤30mg/ml in DMSO;50mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

galacto-Dapagliflozin

Background

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DDMS

PDM 11

γ-Linolenic Acid methyl ester