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| 品牌 | absin | CAS | 864070-44-0 |
|---|---|---|---|
| 分子式 | C23H27ClO7 | 纯度 | 99% |
| 分子量 | 450.91 | 货号 | abs47027853 |
| 规格 | 50mg | 供货周期 | 现货 |
| 主要用途 | is a potent | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Empagliflozin 864070-44-0
| 产品描述 | |
| 描述 | Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. |
| 纯度 | 99% |
| 储存/保存方法 | Store at -20℃ for three years（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 依帕列净；恩ge列净；BI-10773；BI 10773；BI10773 |
| 外观 | White to off white solid |
| 可溶性/溶解性 | DMSO : 83 mg/mL (184.1 mM) |
| 生物活性 | |
| 靶点 | SGLT2 |
| In vitro(体外研究) | Empagliflozin shows >2500-fold selectivity for hSGLT-2 over hSGLT-1 (IC50 8300 nM) and >3500-fold selectivity over hSGLT-4, it exhibits >350-fold selectivity over hSGLT-5 (IC50=1100 nM) and >600-fold selectivity over hSGLT-6. No relevant inhibition of GLUT1 is observed up to 10 μM Empagliflozin. In a kinetic binding experiments, -empagliflozin displays a high affinity for SGLT-2 with a mean Kd of 57 nM in the absence of glucose, and shows a half-life of -empagliflozin-binding to SGLT-2 of 59 min in the absence of glucose.Its binding to SGLT-2 is competitive with glucose. |
| In vivo(体内研究) | High exposure of empagliflozin is achieved in dogs, with plasma concentrations >100-fold above IC50 measured 24 h after administration of 5 mg/kg empagliflozin. The total plasma clearance of empagliflozin in ZDF rat is 43 mL/min/kg, while in dogs is lower at 1.8 mL/min/kg. Cmax of empagliflozin in ZDF rat and dogs is 167 nM and 17254 nM, respectively. Terminal elimination half-life in ZDF rat and dogs is 1.5 h and 6.3 h, respectively. Bioavailability of empagliflozin in ZDF rat is 33.2%, while in dogs is higher at 89.0%. Long-term treatment with empagliflozin, improves glycaemic controland features of metabolic syndrome in diabetic rats. |
| 研究领域 | |
| 研究领域 | Signal TransductionMetabolismPlasma MembraneChannels Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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