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

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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 413 In-stock
Solution
10 mM * 1 mL in DMSO USD 413 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 580 In-stock
25 mg USD 986 In-stock
50 mg USD 1350 In-stock
100 mg USD 1850 In-stock
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

KGA-2727 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE KGA-2727

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SGLT1 SGLT2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

KGA-2727 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

536.62

Formula

C26H40N4O8
CAS No.
Appearance

Solid

Color

White to yellow

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
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 : 200 mg/mL (372.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

H2O : 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / Ethanol / DMSO 1 mM 1.8635 mL 9.3176 mL 18.6352 mL 46.5879 mL
5 mM 0.3727 mL 1.8635 mL 3.7270 mL 9.3176 mL
10 mM 0.1864 mL 0.9318 mL 1.8635 mL 4.6588 mL
15 mM 0.1242 mL 0.6212 mL 1.2423 mL 3.1059 mL
20 mM 0.0932 mL 0.4659 mL 0.9318 mL 2.3294 mL
25 mM 0.0745 mL 0.3727 mL 0.7454 mL 1.8635 mL
30 mM 0.0621 mL 0.3106 mL 0.6212 mL 1.5529 mL
Ethanol / DMSO 40 mM 0.0466 mL 0.2329 mL 0.4659 mL 1.1647 mL
50 mM 0.0373 mL 0.1864 mL 0.3727 mL 0.9318 mL
60 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7765 mL
80 mM 0.0233 mL 0.1165 mL 0.2329 mL 0.5823 mL
100 mM 0.0186 mL 0.0932 mL 0.1864 mL 0.4659 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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KGA-2727 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KGA-2727666842-36-0KGA2727KGA 2727SGLTSodium-dependent glucose cotransportersSGLT1firstorallyantidiabeticglucoseinsulinhyperglycemiaInhibitorinhibitorinhibit

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