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KGA-2727

Name: KGA-2727
Brand: TargetMol
SKU: T15656
Price: 117 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15656Cas No. 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.

KGA-2727

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Purity: 98.46%

Catalog No. T15656Cas No. 666842-36-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$117	In Stock	In Stock
2 mg	$169	In Stock	In Stock
5 mg	$289	In Stock	In Stock
10 mg	$478	In Stock	In Stock
25 mg	$789	In Stock	In Stock
50 mg	$1,080	In Stock	In Stock
100 mg	$1,480	-	In Stock
1 mL x 10 mM (in DMSO)	$339	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.46%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

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	SGLT1 (human):(ki)97.4 nM, SGLT1 (rat):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.

Chemical Properties

Molecular Weight	536.62
Formula	C₂₆H₄₀N₄O₈
Cas No.	666842-36-0
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
Relative Density.	1.308 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

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

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.32 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8635 mL	9.3176 mL	18.6352 mL	93.1758 mL
5 mM	0.3727 mL	1.8635 mL	3.7270 mL	18.6352 mL
10 mM	0.1864 mL	0.9318 mL	1.8635 mL	9.3176 mL
20 mM	0.0932 mL	0.4659 mL	0.9318 mL	4.6588 mL
50 mM	0.0373 mL	0.1864 mL	0.3727 mL	1.8635 mL
100 mM	0.0186 mL	0.0932 mL	0.1864 mL	0.9318 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc