Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KGA-2727 is a potent and selective SGLT1 inhibitor, with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 for the treatment of diabete.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 135.00 | |
2 mg | In stock | $ 193.00 | |
5 mg | In stock | $ 289.00 | |
10 mg | In stock | $ 478.00 | |
25 mg | In stock | $ 789.00 | |
50 mg | In stock | $ 1,080.00 | |
100 mg | In stock | $ 1,480.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 339.00 |
Description | KGA-2727 is a potent and selective SGLT1 inhibitor, with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 for the treatment of diabete. |
Targets&IC50 | hSGLT1:(ki)97.4 nM, rat SGLT1:43.5 nM(ki) |
In vitro | KGA-2727, which has a pyrazole-O-glucoside structure, as the first selective SGLT1 inhibitor.?KGA-2727 inhibited SGLT1 potently and highly selectively in an in vitro assay using cells transiently expressing recombinant SGLTs.KGA2727 dose-dependently inhibits Methyl-Dglucopyranoside (AMG) uptake by SGLT1 and SGLT2.?A Dixon plot analysis for KGA-2727 shows good linearity for human SGLT1 and SGLT2.?KGA-2727 inhibits these SGLTs in a competitive manner displayed from the results of the Dixon plot. |
In vivo | In a small intestine closed loop absorption test with normal rats, KGA-2727 inhibited the absorption of glucose but not that of fructose.?After oral intake of starch along with KGA-2727 in normal rats, the residual content of glucose in the gastrointestinal tract increased.?In the oral glucose tolerance test with streptozotocin-induced diabetic rats, KGA-2727 attenuated the elevation of plasma glucose after glucose loading, indicating that KGA-2727 improved postprandial hyperglycemia.?In Zucker diabetic fatty (ZDF) rats, chronic treatments with KGA-2727 reduced the levels of plasma glucose and glycated hemoglobin.?Furthermore, KGA-2727 preserved glucose-stimulated insulin secretion and reduced urinary glucose excretion with improved morphological changes of pancreatic islets and renal distal tubules in ZDF rats.?In addition, the chronic treatment with KGA-2727 increased the level of glucagon-like peptide-1 in the portal vein. |
Molecular Weight | 536.62 |
Formula | C26H40N4O8 |
CAS No. | 666842-36-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (186.35 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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