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Empagliflozin

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Chemical Structure| 864070-44-0 同义名 : 依帕列净 (BI 10773) ;BI 10773
CAS号 : 864070-44-0
货号 : A112500
分子式 : C23H27ClO7
纯度 : 98%
分子量 : 450.91
MDL号 : -
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(110.89 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

15% Captisol+water 15 mg/mL suspension

生物活性
靶点

  • SGLT2

    SGLT2, IC50:3.1 nM
描述 Sodium glucose cotransporter-2 (SGLT-2) is responsible for glucose reabsorption via the kidney. Empagliflozin is a selective SGLT-2 inhibitor that blocks the uptake of [14C]-AMG via human SGLT-2 (hSGLT-2) with an IC50 value of 3.1nM in vitro. It exhibited >2500-, >3500-, >350-, and >600-fold selectivity over hSGLT-1 (IC50 = 8.3μM), hSGLT-4 (IC50 = 11μM), hSGLT-5 (IC50 = 1.1μM), and hSGLT-6 (IC50 = 2.0μM), respectively. In kinetic binding experiments, [3H]-empagliflozin showed a high affinity for SGLT-2 (Kd = 57nM) in the absence of glucose, whereas glucose at 20nM lowered the affinity of empagliflozin to a Kd value of 194nM[8]. In db/db mice, treatment with empagliflozin (10mg/kg/day in food) for 4 weeks decreased the ventricular mass, lowered the fasting glucose level and elevated the fed and fasted ketone levels as compared to the vehicle-treated group. In the presence of insulin, empagliflozin-treated db/db mice showed increased mean palmitate oxidation rate in the heart in comparison to C57BL/6J mice. The cardiac ATP production rate in vehicle-treated db/db mice was 36% lower than that in C57BL/6J mice, whereas empagliflozin treatment restored the ATP production rate to the level similar to that in C57BL/6J mice[9].
作用机制 Empagliflozin is a potent and selective inhibitor of SGLT-2. It binds to SGLT-2 in a glucose-competitive manner[8].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.09mL

2.22mL

1.11mL

22.18mL

4.44mL

2.22mL
参考文献

[1]Panchapakesan U, Pegg K, et al. Effects of SGLT2 inhibition in human kidney proximal tubular cells--renoprotection in diabetic nephropathy? PLoS One. 2013;8(2):e54442.

[2]Thomas L, Grempler R, et al. Long-term treatment with empagliflozin, a novel, potent and selective SGLT-2 inhibitor, improves glycaemic control and features of metabolic syndrome in diabetic rats. Diabetes Obes Metab. 2012 Jan;14(1):94-6.

[3]Lee KA, Jin HY, et al. Effect of Empagliflozin, a Selective Sodium-Glucose Cotransporter 2 Inhibitor, on Kidney and Peripheral Nerves in Streptozotocin-Induced Diabetic Rats. Diabetes Metab J. 2018 Aug;42(4):338-342.

[4]Shao Q, Meng L, et al. Empagliflozin, a sodium glucose co-transporter-2 inhibitor, alleviates atrial remodeling and improves mitochondrial function in high-fat diet/streptozotocin-induced diabetic rats. Cardiovasc Diabetol. 2019 Nov 28;18(1):165.

[5]Cheng ST, Chen L, et al. The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic β-Cell Mass and Glucose Homeostasis in Type 1 Diabetes. PLoS One. 2016 Jan 25;11(1):e0147391.

[6]Pennig J, Scherrer P, et al. Glucose lowering by SGLT2-inhibitor empagliflozin accelerates atherosclerosis regression in hyperglycemic STZ-diabetic mice. Sci Rep. 2019 Nov 29;9(1):17937.

[7]Empagliflozin

[8]Grempler R, Thomas L, Eckhardt M, Himmelsbach F, Sauer A, Sharp DE, Bakker RA, Mark M, Klein T, Eickelmann P. Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab. 2012 Jan;14(1):83-90.

[9]Verma S, Rawat S, Ho KL, Wagg CS, Zhang L, Teoh H, Dyck JE, Uddin GM, Oudit GY, Mayoux E, Lehrke M, Marx N, Lopaschuk GD. Empagliflozin Increases Cardiac Energy Production in Diabetes: Novel Translational Insights Into the Heart Failure Benefits of SGLT2 Inhibitors. JACC Basic Transl Sci. 2018 Aug 26;3(5):575-587.