| 产品描述: | 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 proagent based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models |
| 靶点: |
hSGLT2:1.95 μM (Ki);rSGLT2:2.14 μM (Ki);hSGLT1:43.1 μM (Ki);rSGLT1:8.57 μM (Ki);SGLT |
| 体内研究: |
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. 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. 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. 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). Animal Model: db/db mice at the age of 8 weeks 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. |
| 参考文献: |
1. Yoshikazu Fujimori, et al. Remogliflozin Etabonate, in a Novel Category of Selective Low-Affinity Sodium Glucose Cotransporter (SGLT2) Inhibitors, Exhibits Antidiabetic Efficacy in Rodent Models. J Pharmacol Exp Ther. 2008 Oct;327(1):268-76. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.914 ml |
9.568 ml |
19.136 ml |
| 5 mM |
0.383 ml |
1.914 ml |
3.827 ml |
| 10 mM |
0.191 ml |
0.957 ml |
1.914 ml |
| 50 mM |
0.038 ml |
0.191 ml |
0.383 ml |
|
| 注意: |
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