1. Membrane Transporter/Ion Channel
  2. SGLT
  3. Remogliflozin etabonate

Remogliflozin etabonate (Synonyms: GSK189075)

Cat. No.: HY-14945 Purity: 99.47%
Handling Instructions

Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a prodrug based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.

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

Remogliflozin etabonate Chemical Structure

Remogliflozin etabonate Chemical Structure

CAS No. : 442201-24-3

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10 mM * 1 mL in DMSO USD 149 In-stock
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100 mg USD 1080 In-stock
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Description

Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a prodrug based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models[1].

IC50 & Target[1]

hSGLT2

1.95 μM (Ki)

rSGLT2

2.14 μM (Ki)

hSGLT1

43.1 μM (Ki)

rSGLT1

8.57 μM (Ki)

In Vivo

Remogliflozin etabonate (GSK189075; 10 or 30 mg/kg; orally; twice daily for 6 weeks) significantly reduced both the FPG and GHb levels in a dosedependent manner[1].
Remogliflozin etabonate (3, 10, 30 mg/kg; orally) increases urinary glucose excretion in a dose-dependent manner. Remogliflozin etabonate dose-dependently inhibits the increase in plasma glucose after glucose loading and decreases the plasma insulin in normal rats[1].
Remogliflozin etabonate (1-10 mg/kg; orally) decreases the blood glucose and reduces the AUC0–6 h for blood glucose in a dose-dependent manner[1].
Remogliflozin etabonate (high-fat diet containing 0.01, 0.03, or 0.1% remogliflozin etabonate for 8 weeks) reduces the levels of plasma glucose, plasma insulin, and GHb in a dose-dependent manner, and it suppresses the development of hypertriglyceridemia in male GK rats (6 weeks of age)[1].

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

Animal Model: db/db mice at the age of 8 weeks[1]
Dosage: 10 or 30 mg/kg
Administration: Orally; twice daily for 6 weeks
Result: Significantly reduced both the fasting plasma glucose (FPG) and glycated hemoglobin (GHb) levels in a dosedependent manner.
Reduced both urine volume and urinary glucose excretion with ameliorated the hyperglycemia.
Clinical Trial
Molecular Weight

522.59

Formula

C26H38N2O9

CAS No.
SMILES

CCOC(OC[[email protected]]1O[[email protected]]([[email protected]@H]([[email protected]@H](O)[[email protected]@H]1O)O)OC2=NN(C(C)C)C(C)=C2CC3=CC=C(OC(C)C)C=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (191.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9135 mL 9.5677 mL 19.1355 mL
5 mM 0.3827 mL 1.9135 mL 3.8271 mL
10 mM 0.1914 mL 0.9568 mL 1.9135 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: ≥ 2.5 mg/mL (4.78 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution

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

Purity: 99.47%

References
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Product Name:
Remogliflozin etabonate
Cat. No.:
HY-14945
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