Home GPCR & G Protein SGLT inhibitor KGA-2727 For research use only.

KGA-2727

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.

KGA-2727 Chemical Structure

KGA-2727 Chemical Structure

CAS: 666842-36-0

Purity & Quality Control

Batch: S893801 DMSO] 100 mg/mL] false] Water] 100 mg/mL] false] Ethanol] 45 mg/mL] false Purity: 99.75%
99.75

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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
In vitro

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

Chemical lnformation & Solubility

Molecular Weight 536.62 Formula

C26H40N4O8
CAS No. 666842-36-0 SDF --
Smiles CC1=C(C=CC(=C1)OCCCNCCC(=O)N)CC2=C(NN=C2OC3C(C(C(C(O3)CO)O)O)O)C(C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (186.35 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 45 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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