[CAS NO. 442201-24-3] Remogliflozinetabonate
PRODUCTS SPECIFICATIONS [442201-24-3]
DESCRIPTION [442201-24-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 522.59 |
| Molecular Formula | C26H38N2O9 |
| SMILES | CCOC(OC[C@H]1O[C@H]([C@@H]([C@@H](O)[C@@H]1O)O)OC2=NN(C(C)C)C(C)=C2CC3=CC=C(OC(C)C)C=C3)=O |
Summary
Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with K i 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
|
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 AUC
0–6 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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00500331 | GlaxoSmithKline |
Diabetes Mellitus, Type 2
|
January 23, 2007 | Phase 2 |
| NCT00501930 | GlaxoSmithKline |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2
|
April 2007 | Phase 1 |
| NCT00559884 | GlaxoSmithKline |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2
|
November 2007 | Phase 1 |
| NCT00532610 | GlaxoSmithKline |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2
|
September 2007 | Phase 1 |
| NCT00501397 | GlaxoSmithKline |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2
|
February 2007 | Phase 1 |
| NCT00376038 | GlaxoSmithKline |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2
|
August 2006 | Phase 1 |
| NCT00494767 | GlaxoSmithKline |
Diabetes Mellitus, Type 2|Obesity
|
September 29, 2006 | Phase 1 |
| NCT00501683 | GlaxoSmithKline |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2
|
November 2006 | Phase 1 |
| NCT00519480 | GlaxoSmithKline |
Diabetes Mellitus, Type 2
|
September 11, 2007 | Phase 1 |
| NCT00495469 | GlaxoSmithKline |
Diabetes Mellitus, Type 2
|
August 17, 2007 | Phase 2 |
| NCT02537470 | BHV Pharma|Integrium |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2
|
July 2015 | Phase 2 |
| NCT00625859 | GlaxoSmithKline |
Diabetes Mellitus, Type 2
|
January 16, 2008 | Phase 1 |
| NCT00575159 | GlaxoSmithKline |
Diabetes Mellitus, Type 1
|
March 31, 2008 | Phase 2 |
| NCT00671424 | GlaxoSmithKline |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2
|
March 2008 | Phase 1 |
| NCT00504816 | GlaxoSmithKline |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2
|
April 2007 | Phase 1 |
| NCT00291356 | GlaxoSmithKline |
Diabetes Mellitus, Type 2|Non-Insulin-Dependent Diabetes Mellitus
|
January 2006 | Phase 2 |
| NCT00501462 | GlaxoSmithKline |
Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2|Renal Insufficiency
|
July 2007 | Phase 1 |
Appearance
Solid
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
DMSO : 100 mg/mL ( 191.35 mM ; Need ultrasonic)
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 |
Synonyms