Empagliflozin (BI 10773)
(Synonyms: 恩格列净; BI 10773) 目录号 : GC16212
An SGLT2 inhibitor
Cas No.:864070-44-0
Sample solution is provided at 25 µL, 10mM.
Empagliflozin is a selective inhibitor of SGLT-2 with IC50 value of 3.1 nM [1].
Sodium glucose cotransporter-2 (SGLT-2) is a member of sodium glucose co-transporter family and plays a pivotal role in glucose reabsorption in the kidney [2].
Empagliflozin is a potent SGLT-2 inhibitor and has a high degree of selectivity over SGLT-1, 4, 5 and 6 than other reported SGLT-2 inhibitors. When tested with a panel of human cell lines over-expressed SGLT-1, 2, 4, 5 and 6, Empagliflozin treatment competitively bind to SGLT-2 over glucose at low dose [1]. In human proximal tublular cell (PTC) cell line HK2 cells, Empagliflozin treatment for 72 h inhibits the expression of SGLT-2 which in turn reversed high glucose induced TLR4 expression, NF-κB binding, IL-6 secretion, AP-1 binding and CIV expression [3].
In Zucker diabetic fatty rat model, oral administration of Empagliflozin shows good efficiency with moderate total plasma clearance (CL) and bioavailability (BA) which indicated that Empagliflozin as an innovative therapeutic approach to treat diabetes in clinic [1]. When treated Zucker diabetic fatty rat model with Empagliflozin, both single and multiple doses results in the urinary glucose excretion and reductions in blood glucose levels [4].
References:
[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.
| Cell experiment [1]: | |
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Cell lines |
HK2 cells |
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Preparation method |
The solubility of this compound in DMSO is > 20.75 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
100 or 500 nM; 72 hrs |
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Applications |
In HK2 cells, Empagliflozin blocked SGLT2 without causing a compensatory increase in the other glucose transporters. Empagliflozin at both concentrations significantly inhibited high glucose-induced TLR4 expression by 97.2 ± 8.2% and 64.4 ± 12.6%, respectively. Besides, at the dose of 500 nM, Empagliflozin significantly inhibited high glucose-induced NF- κB binding by 91.7 ± 14.9%. In addition, Empagliflozin reduced high glucose-induced secretion of IL-6 by 92.0 ± 11.7% and 116.5 ± 19.6% at the doses of 100 and 500 nM, respectively. |
| Animal experiment [2]: | |
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Animal models |
ZDF rats and beagle dogs |
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Dosage form |
2 mL/kg; i.v. or p.o. |
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Applications |
Empagliflozin achieved high exposure in dogs, with plasma concentrations > 100-fold above the IC50 value (measured 24 hrs after administration). In ZDF rat, the total plasma clearance of Empagliflozin was 43 mL/min/kg, while in dogs, was lower at 1.8 mL/min/kg. The Cmax values of Empagliflozin for ZDF rat and dogs were 167 nM and 17254 nM, respectively. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| Cas No. | 864070-44-0 | SDF | |
| 别名 | 恩格列净; BI 10773 | ||
| 化学名 | (2S,3R,4R,5S,6R)-2-[4-chloro-3-[[4-[(3S)-oxolan-3-yl]oxyphenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol | ||
| Canonical SMILES | C1COCC1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)Cl | ||
| 分子式 | C23H27ClO7 | 分子量 | 450.91 |
| 溶解度 | ≥ 20.75mg/mL in DMSO, ≥ 7.06 mg/mL in EtOH with ultrasonic | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2177 mL | 11.0887 mL | 22.1774 mL |
| 5 mM | 0.4435 mL | 2.2177 mL | 4.4355 mL |
| 10 mM | 0.2218 mL | 1.1089 mL | 2.2177 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
