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KGA-2727

Catalog No. T15656   CAS 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.

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KGA-2727 Chemical Structure
KGA-2727, CAS 666842-36-0
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
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Purity: 98.95%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (186.35 mM), sonification is recommended.

TargetMolReferences and Literature

1. Shibazaki T, et al. KGA-2727, a novel selective inhibitor of a high-affinity sodium glucose cotransporter (SGLT1), exhibits antidiabetic efficacy in rodent models. J Pharmacol Exp Ther. 2012 Aug;342(2):288-96.

Related compound libraries

This product is contained In the following compound libraries:
NO PAINS Compound Library Glycometabolism Compound Library Ion Channel Inhibitor Library Bioactive Compounds Library Max Anti-Diabetic Compound Library Metabolism Compound Library GPCR Compound Library Inhibitor Library Bioactive Compound Library Orally Active Compound Library

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Keywords

KGA-2727 666842-36-0 GPCR/G Protein SGLT insulin inhibit Sodium-dependent glucose cotransporters hyperglycemia KGA2727 antidiabetic first glucose KGA 2727 Inhibitor SGLT1 orally inhibitor

 

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