[CAS NO. 666842-36-0] KGA-2727

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PRODUCTS SPECIFICATIONS [666842-36-0]

Catalog

HY-123797

Brand

MCE

CAS

666842-36-0

DESCRIPTION [666842-36-0]

Overview

MDL	-
Molecular Weight	536.62
Molecular Formula	C26H40N4O8
SMILES	O=C(N)CCNCCCOC1=CC=C(CC2=C(C(C)C)NN=C2O[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO)O3)O)O)O)C(C)=C1

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

Summary

KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with K _i s of 97.4 nM and 43.5 nM for human and rat SGLT1 , respectively. The selectivity ratios ( K _i for SGLT2/ K _i 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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

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)

H ₂ O : 20 mg/mL ( 37.27 mM ; ultrasonic and warming and heat to 60°C)

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: ≥ 5 mg/mL (9.32 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 5 mg/mL (9.32 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 5 mg/mL (9.32 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Shibazaki T, et al. KGA-2727, a novel selective inhibitor of a high-affinity sodium glucose cotransporter (SGLT1), exhibits antidiabetic efficacy in rodent models. J Pharmacol Exp Ther. 2012 Aug;342(2):288-96.

Synonyms

Propanamide, 3-[[3-[4-[[3-(β-D-glucopyranosyloxy)-5-(1-methylethyl)-1H-pyrazol-4-yl]methyl]-3-methylphenoxy]propyl]amino]-

3-[[3-[4-[[3-(β-D-Glucopyranosyloxy)-5-(1-methylethyl)-1H-pyrazol-4-yl]methyl]-3-methylphenoxy]propyl]amino]propanamide