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Empagliflozin

依帕列净,恩格列嗪,艾帕列净,恩格列净,BI-10773

Empagliflozin (BI 10773)是一种有效的，选择性SGLT-2抑制剂，IC50为3.1 nM，比作用于SGLT-1， 4， 5和6选择性高300倍以上。

目录号
EY0853
EY0853
EY0853
EY0853
纯度
99.16%
99.16%
99.16%
99.16%
规格
5 mg
10 mg
50 mg
100 mg
原价
360
540
705
945
售价
360
540
705
945
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    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. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~ 500 Nm

  • 动物实验

    ~2 mL/kg静脉注射或口服处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Grempler R, et al. Diabetes Obes Metab, 2012, 14(1), 83-90.
    [2] Luippold G, Klein T, Mark M, Grempler R. Empagliflozin, a novel potent and selective SGLT-2 inhibitor, improves glycaemic control alone and in combination with insulin in streptozotocin-induced diabetic rats, a model of type 1 diabetes mellitus. Diabetes Obes Metab. 2012 Jul;14(7):601-7.
    [3] Thomas L, Grempler R, Eckhardt M 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.

    分子式
    C23H27ClO7    		 分子量
    450.91    		 CAS号
    864070-44-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    86 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT03030222 Heart Failure Drug: Empagliflozin 10Mg Tab|Drug: Placebo Oral Tablet Saint Luke's Health System Phase 4 2017-03-01 2017-03-01
    NCT02686476 Non Alcoholic Fatty Liver Disease Drug: Empagliflozin Medanta, The Medicity, India 2016-03-01 2016-12-18
    NCT02932436 Diabetes Mellitus, Type 2|Diastolic Dysfunction Drug: Empagliflozin|Drug: Placebo Johannes Gutenberg University Mainz|Boehringer Ingelheim Phase 4 2016-10-01 2016-11-08
    NCT03059056 Diabetes Mellitus Drug: Empagliflozin 25mg British University In Egypt Phase 1 2017-02-02 2017-02-16
    NCT03008551 Polycystic Ovary Syndrome Drug: Empagliflozin|Drug: Metformin University of Hull Phase 2|Phase 3 2017-06-01 2017-03-23
    NCT02998970 Diabetes|Cardiovascular Disease Drug: Empagliflozin|Drug: Placebo St. Michael's Hospital, Toronto|Boehringer Ingelheim (Canada) LTD Phase 4 2017-01-01 2017-01-31
    NCT03087773 Acute Myocardial Infarction Drug: Empagliflozin 10 mg|Drug: Placebo Oral Tablet Medical University of Graz|United Arab Emirates University|Medical University of Vienna|Landeskrankenhaus Feldkirch|Krankenhaus der Barmherzigen Br眉der Linz|Kepler University Hospital|Paracelsus Medical University Phase 3 2017-05-02 2017-03-22
    NCT02637973 Type 2 Diabetes|Non-alcoholic Fatty Liver Disease Drug: Empagliflozin|Drug: Placebo The Deutsche Diabetes Forschungsgesellschaft e.V.|Boehringer Ingelheim|German Diabetes Center Phase 4 2015-12-01 2016-12-14
    NCT02632747 Diabetes Mellitus, Type 1 Drug: Empagliflozin|Drug: Placebo (matching empagliflozin)|Drug: ramipril Boehringer Ingelheim|Eli Lilly and Company Phase 2 2016-05-01 2017-03-17
    NCT03078101 Diabetic Kidney Disease|Diabetes Mellitus, Type 2|Chronic Kidney Disease stage3|Chronic Kidney Disease stage4 Drug: Empagliflozin 10 MG [Jardiance]|Drug: Placebo Oral Tablet Medical University of Vienna|Attoquant Diagnostics Phase 2 2017-03-01 2017-03-07
    NCT02964715 Type2 Diabetes|NAFLD Drug: Empagliflozin University of Malaya Phase 4 2016-11-01 2016-11-24
    NCT02815644 Healthy Drug: empagliflozin/linagliptin FDC Boehringer Ingelheim Phase 1 2016-07-01 2017-02-07
    NCT02577315 Healthy Drug: Empagliflozin|Drug: Metformin|Drug: Empagliflozin|Drug: Metformin Boehringer Ingelheim Phase 1 2015-09-01 2016-10-07
    NCT01001962 Hypertension|Type II Diabetes Drug: empagliflozin|Drug: Metformin Aristotle University Of Thessaloniki Phase 4 2016-01-01 2015-04-06
    NCT02230995 Healthy Drug: metformin|Drug: empagliflozin/metformin|Drug: empagliflozin Boehringer Ingelheim|Eli Lilly and Company Phase 1 2014-09-01 2017-01-19
    NCT02266472 Healthy Drug: metformin|Drug: empagliflozin/metformin|Drug: empagliflozin Boehringer Ingelheim|Eli Lilly and Company Phase 1 2014-11-01 2017-01-19
    NCT02848833 Diabetes Mellitus, Type 2 Drug: JARDIANCE 10mg|Drug: JARDIANCE 25mg Boehringer Ingelheim 2016-08-01 2017-03-21
    NCT02758171 Healthy Drug: Empagliflozin|Drug: Linagliptin Boehringer Ingelheim|Eli Lilly and Company Phase 1 2016-05-01 2016-08-10
    NCT02854748 Diabetes Mellitus, Type II Drug: Empagliflozin 25mg|Drug: Lobeglitazone 0.5mg|Drug: Empagliflozin 25mg/Lobeglitazone 0.5mg Chong Kun Dang Pharmaceutical Phase 1 2016-08-01 2016-08-07
    NCT02890745 Diabetes Mellitus, Type 2 Drug: Empagliflozin|Drug: Placebo Henrik Enghusen Poulsen|University Hospital, Gentofte, Copenhagen|University of Copenhagen|Rigshospitalet, Denmark Phase 2 2016-11-01 2016-12-01
    NCT02798744 Diabetes Mellitus, Type 2 Drug: Empagliflozin|Behavioral: Diet|Drug: Placebo University of Leicester|Loughborough University|University Hospitals, Leicester Phase 4 2016-09-01 2016-08-04

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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