442201-24-3
442201-24-3 structure
- Name: Remogliflozin etabonate
- Chemical Name: ethyl [(2R,3S,4S,5R,6S)-3,4,5-trihydroxy-6-[5-methyl-1-propan-2-yl-4-[(4-propan-2-yloxyphenyl)methyl]pyrazol-3-yl]oxyoxan-2-yl]methyl carbonate
- CAS Number: 442201-24-3
- Molecular Formula: C26H38N2O9
- Molecular Weight: 522.58800
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel SGLT
- Create Date: 2016-08-25 05:01:40
- Modify Date: 2024-01-10 16:15:31
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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].
| Name | ethyl [(2R,3S,4S,5R,6S)-3,4,5-trihydroxy-6-[5-methyl-1-propan-2-yl-4-[(4-propan-2-yloxyphenyl)methyl]pyrazol-3-yl]oxyoxan-2-yl]methyl carbonate |
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| Synonyms |
remogliflozin etabonate
UNII-TR0QT6QSUL Remogliflozin etabonate (USAN/INN) KGT-1681 |
| 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]. |
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| Related Catalog | |
| Target |
hSGLT1:43.1 μM (Ki) rSGLT1:8.57 μM (Ki) hSGLT2:1.95 μM (Ki) rSGLT2:2.14 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]. 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. |
| References |
| Molecular Formula | C26H38N2O9 |
|---|---|
| Molecular Weight | 522.58800 |
| Exact Mass | 522.25800 |
| PSA | 141.73000 |
| LogP | 2.50990 |
| Storage condition | 2-8°C |