S82012 |
Bexagliflozin |
源叶(MedMol) | ≥97% |
- 提示:详情请下载说明书。
- 产品描述: EGT1442 is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 5.6 μM and 2 nM for human SGLT1 and SGLT2, respectively
- 靶点: SGLT
- 体内研究:
EGT1442 produces a stable urinary excretion of glucose in rats and dogs with ED50 values of 0.38 and 0.09 mg/kg, respectively, and reduces HbA(1c) and blood glucose in db/db mice in a concentration dependent manner.
- 动物实验: Prior to experiment initiation, 7-week old SHRSP rats were assigned to 3 groups of 15 males each, based on body weights. During this week, daily water consumption was determined in order to calculate appropriate drug concentrations for the drinking water. The following week (Day 1), rats were switched to a stroke-promoting diet containing reduced potassium and protein and elevated NaCl. Animals received water bottles containing either no compound, EGT1442 (3.0 mg/kg) or the sodium channel blocker amiloride (1.0 mg/kg). Body weights were measured 2 times per week, and dosages were adjusted weekly. Water consumption was likewise measured 2 times per week, while food consumption wasmeasured weekly. Daily values were estimated. Urine samples were analyzed by test strips once every two weeks. Additionally, all animals were observed twice daily and any abnormal findings were recorded.
- 参考文献:
1. Zhang W , Welihinda A , Mechanic J , et al. EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA1c levels in db/db mice and prolongs the survival of stroke-prone rats[J]. Pharmacological Research, 2011, 63(4):284-293.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.151 ml 10.754 ml 21.508 ml 5 mM 0.43 ml 2.151 ml 4.302 ml 10 mM 0.215 ml 1.075 ml 2.151 ml 50 mM 0.043 ml 0.215 ml 0.43 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)