Empagliflozin

製品コードS8022 バッチS802202

印刷

化学情報

Chemical Structure Synonyms BI 10773 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H27ClO7
分子量 450.91 CAS No. 864070-44-0
Solubility (25°C)* 体外 DMSO 90 mg/mL (199.59 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Empagliflozin 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. Phase 3.
in vitro 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, [3H]-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 [3H]-empagliflozin-binding to SGLT-2 of 59 min in the absence of glucose.Its binding to SGLT-2 is competitive with glucose. [1]
in vivo 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. [1] 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 control and features of metabolic syndrome in diabetic rats. [2]

プロトコル(参考用のみ)

キナーゼアッセイ [14C]-monosaccharide uptake inhibition experiments
Stable cell lines over-expressing hSGLT-1, -2, -4, -5 or -6 or rSGLT-1 or -2 are used for the sodium-dependent monosaccharide transport inhibition assay. Cells are pre-incubated in 200 μL uptake buffer (10 mM HEPES, 137 mM NaCl, 5.4 mM KCl, 2.8 mM CaCl2, 1.2 mM MgCl2, 50 μg/ml Gentamycin, 0.1% BSA) for 25 minutes at 37°C. 10 μM Cytochalasin B and test compound is added at different concentrations 15 minutes before the initiation of the uptake experiment. The uptake reaction is started by the addition of 0.6 μCi [14C]-labelled monosaccharide i.e. [14C]-labelled AMG, glucose, fructose, mannose or myo-inositol, in 0.1 mM AMG (or the respective non-radioactive monosaccharide). After incubation for 60 minutes (hSGLT-5), 90 minutes (hSGLT-4) or 4 hours (hSGLT-2) at 37°C, the cells are washed three times with 300 μL PBS and then lysed in 0.1 N NaOH with intermittent shaking for 5 minutes. The lysate is mixed with 200 μL MicroScint 40 and shaken for 15 minutes and counted for radioactivity in the TopCount NXT. For SGLT-4 and SGLT-5 assays cells are pre-incubated in pre-treatment buffer (uptake buffer containing choline chloride instead of NaCl) for 25 minutes prior to addition of uptake buffer.
細胞アッセイ 細胞株 HK2 cells (human kidney PTC line)
濃度 ~ 500 nM
反応時間 72 h
実験の流れ MTS assay
動物実験 動物モデル ZDF rats and beagle dogs
投薬量 ~2 mL/kg
投与方法 Intravenously or orally

カスタマーフィードバック

Data from [Data independently produced by , , Diabetes, 2016, 65(9):2784-94]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Empagliflozin improves mitochondrial dysfunction in diabetic cardiomyopathy by modulating ketone body metabolism and oxidative stress [ Redox Biol, 2024, 69:103010] PubMed: 38160540
Kidney glycolysis serves as a mammalian phosphate sensor that maintains phosphate homeostasis [ J Clin Invest, 2023, 133(8)e164610] PubMed: 36821389
Empagliflozin targets Mfn1 and Opa1 to attenuate microglia-mediated neuroinflammation in retinal ischemia and reperfusion injury [ J Neuroinflammation, 2023, 20(1):296] PubMed: 38082266
Targeting high glucose-induced epigenetic modifications at cardiac level: the role of SGLT2 and SGLT2 inhibitors [ Cardiovasc Diabetol, 2023, 22(1):24] PubMed: 36732760
Empagliflozin reduces podocyte lipotoxicity in experimental Alport syndrome [ Elife, 2023, 12e83353] PubMed: 37129368
Multi-omics analysis reveals attenuation of cellular stress by empagliflozin in high glucose-treated human cardiomyocytes [ J Transl Med, 2023, 21(1):662] PubMed: 37742032
Multi-omics analysis reveals attenuation of cellular stress by empagliflozin in high glucose-treated human cardiomyocytes [ J Transl Med, 2023, 21(1):662] PubMed: 37742032
Targeting unfolded protein response reverts ER stress and ER Ca2+ homeostasis in cardiomyocytes expressing the pathogenic variant of Lamin A/C R321X [ J Transl Med, 2023, 21(1):340] PubMed: 37217929
The impact of SGLT2 inhibitors on αKlotho in renal MDCK and HK-2 cells [ Front Endocrinol (Lausanne), 2023, 14:1069715] PubMed: 36967770
Empagliflozin Reverses Oxidized LDL-Induced RECK Suppression, Cardiotrophin-1 Expression, MMP Activation, and Human Aortic Smooth Muscle Cell Proliferation and Migration [ Mediators Inflamm, 2023, 2023:6112301] PubMed: 37830075

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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