Empagliflozin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Empagliflozin (BI-10773) 是一种有效的选择性 SGLT-2 抑制剂，IC50 为 3.1 nM。

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.(In Vitro):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 [14C]-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). [3H]-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.(In Vivo):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.

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BI 10773

GPCR/G Protein

SGLT

SGLT1| SGLT2| SGLT4| SGLT5| SGLT6

Metabolic Disease

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864070-44-0

450.91

C23H27ClO7

>98% (HPLC)

DMSO: 90 mg/mL (199.59 mM)

O[C@H]1[C@H](C2=CC=C(Cl)C(CC3=CC=C(O[C@@H]4COCC4)C=C3)=C2)O[C@H](CO)[C@@H](O)[C@@H]1O

(2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol

(-20℃)

With Ice Pack

≥ 2 years