Remogliflozin etabonate GSK189075|cas:442201-24-3|西域试剂

Remogliflozin etabonate GSK189075,99.64%

产品编号：Bellancom-14945| CAS NO：442201-24-3| 分子式：C₂₆H₃₈N₂O₉| 分子量：522.59

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货号	价格	库存与货期
Bellancom-14945	￥1300.00	杭州北京（现货）
Bellancom-14945	￥2100.00	杭州北京（现货）
Bellancom-14945	￥4200.00	杭州北京（现货）
Bellancom-14945	￥6800.00	杭州北京（现货）
Bellancom-14945	￥10800.00	杭州北京（现货）

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Remogliflozin etabonate GSK189075

产品介绍

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 K_i 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体，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。

生物活性

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 proagent based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.

体外研究

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 AUC_{0–6 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).

西域 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
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.

体内研究

西域 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
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.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.78 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.78 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.78 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。