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抑制剂/激活剂

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凋亡与自噬

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Empagliflozin (BI 10773)

Empagliflozin (BI 10773) 恩格列净; BI 10773

Empagliflozin是一种有效的，选择性SGLT-2抑制剂，IC50为3.1 nM，比作用于SGLT-1， 4， 5和6选择性高300倍以上。Phase 3。

货号：
TK0218
规格：

1mg

2mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	864070-44-0
生物活性	Empagliflozin (BI 10773) is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2.
分子式	C23H27ClO7
分子量	450.91
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 50 mg/mL (110.89 mM; Need ultrasonic) H2O : 0.11 mg/mL (0.24 mM; Need ultrasonic and warming)
体内研究	Glucose intolerance is significantly improved after 8 days of Empagliflozin treatment at either dose (3mg/kg Empagliflozin 3058±180 vs 10mg/kg Empagliflozin 3090±219). Therefore, acute treatment with Empagliflozin has a beneficial effect on hyperglycemia and glucose intolerance. Since there are no significant differences in blood glucose homeostasis with the two different doses of Empagliflozin, and random blood glucose levels of T1DM mice are significantly improved by 3mg/kg of Empagliflozin, the effect of the lower dose of Empagliflozin (3mg/kg) is investigated on preserving β-cell mass and function.
体外研究	Empagliflozin is a potent and competitive SGLT-2 inhibitor with an excellent selectivity profile and the highest selectivity window of the tested SGLT-2 inhibitors over hSGLT-1. Empagliflozin inhibits the uptake of [C]-alpha-methyl glucopyranoside (AMG) via hSGLT-2 in a dose-dependent manner with an IC50 of 3.1 nM, but is less potent for other SGLTs (IC50 range: 1100-11000 nM). [H]-Empagliflozin displays a high affinity for SGLT-2 with a mean Kd of 57±37 nM in the absence of glucose in kinetic binding experiments.
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纯度及产品资料	98%

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