KGA-2727

SKU: orb1308156

Description

KGA-2727 is a potent, selective SGLT1 inhibitor with high selectivity over SGLT2. It is a research tool for studying glucose absorption mechanisms in diabetes, applicable in both in vitro binding assays and in vivo metabolic studies.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 666842-36-0
• MW: 536.62
• Purity: 98.95%
• Formula: C₂₆H₄₀N₄O₈
• SMILES: CC(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
• Target: SGLT
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.32 mM);DMSO:100 mg/mL (186.35 mM)

Bioactivity

• Target IC50:
  SGLT1 (rat):43.5 nM(ki)|SGLT1 (human):(ki)97.4 nM
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

antidiabetic, orally, inhibit, KGA 2727, KGA2727, KGA-2727, glucose, hyperglycemia, human SGLT1, first, Inhibitor, insulin, rat SGLT1, SGLT1, SGLT, Sodium-dependent glucose cotransporters

Compound Identifiers

PubChem CID

10052896