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

Remogliflozin etabonate (Synonyms: GSK189075)

目录号: HY-14945 纯度: 99.43%
产品使用指南

Remogliflozin etabonate (GSK189075) 是一种具有口服活性的,选择性和低亲和力的钠葡萄糖共转运蛋白 (SGLT2) 抑制剂,对 hSGLT2,rSGLT2,hSGLT1,rSGLT1 的 Ki 值分别为 1.95 μM,43.1 μM,2.14 μM,8.57 μM。Remogliflozin etabonate 是一种基于苄基吡唑葡糖苷的前药,在体内被代谢成其活性形式,瑞格列净 (Remogliflozin)。Remogliflozin etabonate 在啮齿动物模型中显示出抗糖尿病功效。

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Remogliflozin etabonate Chemical Structure

Remogliflozin etabonate Chemical Structure

CAS No. : 442201-24-3

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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]

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.
Molecular Weight

522.59

Formula

C₂₆H₃₈N₂O₉

CAS No.

442201-24-3

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

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)

References
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Keywords:

Remogliflozin etabonateGSK189075GSK 189075GSK-189075SGLTSodium-dependent glucose cotransportersorallysodiumglucosecotransporterprodrugbenzylpyrazoleglucosideRemogliflozinantidiabeticfastingplasmaFPGglycatedhemoglobinGHbInhibitorinhibitorinhibit

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产品名称:
Remogliflozin etabonate
目录号:
HY-14945
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