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

KGA-2727 

Cat. No.: HY-123797 Purity: 99.04%
COA 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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Solution
10 mM * 1 mL in DMSO USD 413 In-stock
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10 mM * 1 mL
ready for reconstitution
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Solid
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10 mg USD 580 In-stock
25 mg USD 1050 In-stock
50 mg USD 1650 In-stock
100 mg USD 2550 In-stock
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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].

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.
Molecular Weight

536.62

Appearance

Solid

Formula

C26H40N4O8
CAS No.
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)

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
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.
Purity & Documentation
References
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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.

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Keywords:

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

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