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KGA-2727 SGLT inhibitor

Name: KGA-2727
Brand: Selleck Chemicals
SKU: S8938
Rating: 5 (1 reviews)

Cat.No.S8938

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 this compound are 140 (human) and 390 (rat). This chemical exhibits antidiabetic efficacy in rodent models.

Chemical Structure

Molecular Weight: 536.62

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.75

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other SGLT Inhibitors	Sotagliflozin (LX4211) Phlorizin Phloretin (RJC 02792) Tofogliflozin(CSG 452) Ipragliflozin (ASP1941) Mizagliflozin (KWA 0711, DSP-3235 free base) Ipragliflozin L-Proline Bexagliflozin (EGT1442) Swertisin

Chemical Information, Storage & Stability

Molecular Weight	536.62	Formula	C₂₆H₄₀N₄O₈	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	666842-36-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C=CC(=C1)OCCCNCCC(=O)N)CC2=C(NN=C2OC3C(C(C(C(O3)CO)O)O)O)C(C)C

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (186.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 45 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (9.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.71mg/ml (1.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	rat SGLT1 (Cell-free assay) 43.5 nM(Ki) human SGLT1 (Cell-free assay) 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..
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, this compound attenuats the elevation of plasma glucose after glucose loading, indicating that it improves postprandial hyperglycemia. In Zucker diabetic fatty (ZDF) rats, chronic treatments with this chemical reduces the levels of plasma glucose and glycated hemoglobin. Furthermore, it 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 this compound increases the level of glucagon-like peptide-1 in the portal vein..
References	[1] https://pubmed.ncbi.nlm.nih.gov/22537769/

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