Empagliflozin (BI 10773)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Empagliflozin是SGLT-2的选择性抑制剂，IC50值为3.1 nM[1]。
钠葡萄糖共转运体2（SGLT-2）属于钠葡萄糖共转运蛋白家族，在肾脏葡萄糖再吸收过程中发挥关键作用[2]。
Empagliflozin是一种有效的SGLT-2抑制剂，与SGLT-1、4、5和6相比，对SGLT-2具有高度的选择性，比报道的其他SGLT-2抑制剂选择性更强，在一系列过表达SGLT-1、2、4、5和6的人细胞系中，低剂量empagliflozin与葡萄糖竞争结合SGLT-2[1]。在人近端肾小管细胞（PTC）的细胞系HK2细胞中，Empagliflozin治疗72小时抑制SGLT-2的表达，从而逆转高糖诱导的TLR4表达、NF-κB结合、IL-6分泌、AP-1结合以及CIV表达[3]。
在Zucker糖尿病肥胖大鼠模型中，口服empagliflozin产生良好的效率，具有适度的总血浆清除率（CL）和生物利用度（BA），这表明empagliflozin可以作为一种创新的治疗方法用于临床治疗糖尿病[1]。使用empagliflozin处理Zucker糖尿病肥胖大鼠，单剂量和多剂量导致尿糖排泄和血糖水平降低[4]。
参考文献：
[1]. Grempler, R., et al., Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab, 2012. 14(1): p. 83-90.
[2]. Ndefo, U.A., et al., Empagliflozin (Jardiance): A Novel SGLT2 Inhibitor for the Treatment of Type-2 Diabetes. P t, 2015. 40(6): p. 364-8.
[3]. Panchapakesan, U., et al., Effects of SGLT2 inhibition in human kidney proximal tubular cells--renoprotection in diabetic nephropathy PLoS One, 2013. 8(2): p. e54442.
[4]. Thomas, L., 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. 14(1): p. 94-6.
- 1. Cheol Ho Park, Bin Lee, et al. "Canagliflozin protects against cisplatin-induced acute kidney injury by AMPK-mediated autophagy in renal proximal tubular cells." Cell Death Discov. 2022 Jan 10;8(1):12. PMID:35013111
- 2. Zhou Y, Fan J, et al. "SGLT-2 inhibitors reduce glucose absorption from peritoneal dialysis solution by suppressing the activity of SGLT-2." Biomed Pharmacother. 2019 Jan;109:1327-1338. PMID:30551383
- 3. Bahia Abbas Moussa, Marianne Alphonse Mahrouse, et al. "Different resolution techniques for management of overlapped spectra: Application for the determination of novel co-formulated hypoglycemic drugs in their combined pharmaceutical dosage form." Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy Available online 20 June 2018.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 450.91 |
| Cas No. | 864070-44-0 |
| Formula | C23H27ClO7 |
| Solubility | insoluble in H2O; ≥20.75 mg/mL in DMSO; ≥7.06 mg/mL in EtOH with ultrasonic |
| Chemical Name | (2S,3R,4R,5S,6R)-2-[4-chloro-3-[[4-[(3S)-oxolan-3-yl]oxyphenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol |
| SDF | Download SDF |
| Canonical SMILES | C1COCC1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
HK2细胞 |
|
制备方法 |
在DMSO中的溶解度大于20.75 mg/mL。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
|
反应条件 |
100或500 nM；72小时 |
|
实验结果 |
在HK2细胞中，Empagliflozin阻断SGLT2，而不会引起其它葡萄糖转运蛋白的代偿性增加。 在2种浓度下，Empagliflozin显著抑制高浓度葡萄糖诱导的TLR4表达（分别为97.2 ± 8.2%和64.4 ± 12.6%）。在500 nM的剂量下，Empagliflozin显著抑制高浓度葡萄糖诱导的NF-κB结合（91.7 ± 14.9%）。此外，Empagliflozin在100 nM和500 nM的剂量下使高浓度葡萄糖诱导的IL-6分泌分别降低了92.0 ± 11.7%和116.5 ± 19.6%。 |
| 动物实验 [2]: | |
|
动物模型 |
ZDF大鼠和比格犬 |
|
给药剂量 |
2 mL/kg；静脉注射或口服给药 |
|
实验结果 |
Empagliflozin在比格犬中显示出较高的暴露量，其血浆浓度高于IC50值100倍以上（给药后24小时进行测定）。在ZDF大鼠中，Empagliflozin的总血浆清除率为43 mL/min/kg，而在比格犬中，总血浆清除率较低，为1.8 mL/min/kg。Empagliflozin对ZDF大鼠和比格犬的Cmax值分别为167 nM和17254 nM。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Panchapakesan, U., et al., Effects of SGLT2 inhibition in human kidney proximal tubular cells--renoprotection in diabetic nephropathy PLoS One, 2013. 8(2): p. e54442. [2]. Grempler, R., et al., Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab, 2012. 14(1): p. 83-90. |
|
| Description | Empagliflozin (BI 10773) is a selective, potent and dose-depentent inhibitor of SGLT-2(sodium glucose cotransporter-2) with IC50 values of 3.1 nM, 8300 nM, 11000 nM, 1100 nM and 2000 nM, for SGLT-2,1,4,5 and 6, respectively. | |||||
| Targets | SGLT-2 | |||||
| IC50 | 3.1 nM | |||||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
相关生物数据
相关生物数据
