KGA-2727

Catalog No.S8938 Batch:S893801

Print

Technical Data

Formula

C26H40N4O8
Molecular Weight 536.62 CAS No. 666842-36-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (186.35 mM)
Water 100 mg/mL (186.35 mM)
Ethanol 45 mg/mL (83.85 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.
Targets
rat SGLT1 [1]
(Cell-free assay)		 human SGLT1 [1]
(Cell-free assay)
43.5 nM(Ki) 97.4 nM(Ki)
In vitro

KGA-2727 inhibits SGLT1 potently and highly selectively in an in vitro assay using cells transiently expressing recombinant SGLTs.[1].
In vivo

In a small intestine closed loop absorption test with normal rats, KGA-2727 inhibits the absorption of glucose but not that of fructose. In the oral glucose tolerance test with streptozotocininduced diabetic rats, KGA-2727 attenuats the elevation of plasma glucose after glucose loading, indicating that KGA-2727 improves postprandial hyperglycemia. In Zucker diabetic fatty (ZDF) rats, chronic treatments with KGA-2727 reduces the levels of plasma glucose and glycated hemoglobin. Furthermore, KGA-2727 preserves glucose-stimulated insulin secretion and reduces 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 increases the level of glucagon-like peptide-1 in the portal vein.[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    COS-7 cells

  • Concentrations

    0-1 μM, 0-100 μM

  • Incubation Time

    --

  • Method

    For the AMG uptake experiment, COS-7 cells are seeded into a 96-well collagen-coated culture plate at a density of 5 × 104 cells/well in Dulbecco’s modified Eagle’s medium containing 10% fetal bovine serum. After 4 h, each plasmid is transfected into COS-7 cells using Lipofectamine 2000 and the cells are used 2 days after transfection. In this experiment, AMG uptake at 0.3 or 1 mM is measured in the presence of various concentrations of KGA-2727 to calculate Ki values.
Animal Study:

[1]
  • Animal Models

    Male Wistar, Zucker diabetic fatty (ZDF) fa/fa (ZDF/Gmi Crl-fa/fa), and ZDF-lean (ZDF/Gmi Crl-lean) rats

  • Dosages

    10 mg/kg, 30 mg/kg, 100 mg/kg

  • Administration

    Oral gavage

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.