1. Membrane Transporter/Ion Channel
  2. SGLT
  3. KGA-2727

KGA-2727 

Cat. No.: HY-123797 Purity: 99.06%
Handling Instructions

KGA-2727 is a first selective, high-affinity and orally active 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 has antidiabetic efficacy.

For research use only. We do not sell to patients.

KGA-2727 Chemical Structure

KGA-2727 Chemical Structure

CAS No. : 666842-36-0

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5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

KGA-2727 is a first selective, high-affinity and orally active 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 has antidiabetic efficacy[1].

IC50 & Target

Ki: 97.4 nM (human SGLT1), 43.5 nM (rat SGLT1)[1]

In Vitro

A Dixon plot analysis for KGA-2727 displays good linearity for human SGLT1 and SGLT2. The results of the Dixon plot show that KGA-2727 inhibits these SGLTs in a competitive manner. KGA2727 dose-dependently inhibits Methyl-Dglucopyranoside (AMG) uptake by SGLT1 and SGLT2[1].

In Vivo

In the oral glucose tolerance test with streptozotocin-induced diabetic rats, KGA-2727 attenuates the elevation of plasma glucose after glucose loading, indicating that KGA-2727 improves postprandial hyperglycemia[1].
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[1].

Molecular Weight

536.62

Formula

C₂₆H₄₀N₄O₈

CAS No.

666842-36-0

SMILES

O=C(N)CCNCCCOC1=CC=C(CC2=C(C(C)C)NN=C2O[[email protected]]3[[email protected]@H]([[email protected]]([[email protected]@H]([[email protected]@H](CO)O3)O)O)O)C(C)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (186.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8635 mL 9.3176 mL 18.6352 mL
5 mM 0.3727 mL 1.8635 mL 3.7270 mL
10 mM 0.1864 mL 0.9318 mL 1.8635 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

KGA-2727KGA2727KGA 2727SGLTSodium-dependent glucose cotransportersSGLT1firstorallyantidiabeticglucoseinsulinhyperglycemiaInhibitorinhibitorinhibit

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Product Name:
KGA-2727
Cat. No.:
HY-123797
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