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KGA-2727

🥰Excellent
Catalog No. T15656Cas No. 666842-36-0

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.

KGA-2727

KGA-2727

🥰Excellent
Purity: 98.95%
Catalog No. T15656Cas No. 666842-36-0
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 SizePriceAvailabilityQuantity
1 mg$135In Stock
2 mg$193In Stock
5 mg$289In Stock
10 mg$478In Stock
25 mg$789In Stock
50 mg$1,080In Stock
100 mg$1,480In Stock
1 mL x 10 mM (in DMSO)$339In Stock
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Purity:98.95%
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Product Introduction

Bioactivity
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
SGLT1 (human):(ki)97.4 nM, SGLT1 (rat):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.
Chemical Properties
Molecular Weight536.62
FormulaC26H40N4O8
Cas No.666842-36-0
SmilesCC(C)c1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OCCCNCCC(N)=O)cc1C
Relative Density.1.308 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (186.35 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8635 mL9.3176 mL18.6352 mL93.1758 mL
5 mM0.3727 mL1.8635 mL3.7270 mL18.6352 mL
10 mM0.1864 mL0.9318 mL1.8635 mL9.3176 mL
20 mM0.0932 mL0.4659 mL0.9318 mL4.6588 mL
50 mM0.0373 mL0.1864 mL0.3727 mL1.8635 mL
100 mM0.0186 mL0.0932 mL0.1864 mL0.9318 mL

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