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Linagliptin

利拉利汀,BI-1356,BI 1356,Tradjenta

Linagliptin是高活性DPP-4抑制剂，IC50为1 nM，对hERG的亲和力较低。

目录号
EY0950
EY0950
EY0950
纯度
99.61%
99.61%
99.61%
规格
100 mg
500 mg
1 g
原价
450
720
1020
售价
450
720
1020
库存
现货
现货
现货
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  • 生物活性

    Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    ≤1 mg/kg通过口服给药

  • 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] Eckhardt M, et al. J Med Chem. 2007, 50(26), 6450-6453.
    [2] Schürmann C, et al. The dipeptidyl peptidase-4 inhibitor linagliptin attenuates inflammation and accelerates epithelialization in wounds of diabetic ob/ob mice. J Pharmacol Exp Ther. 2012 Jul;342(1):71-80.

    分子式
    C25H28N8O2    		 分子量
    472.54    		 CAS号
    668270-12-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    17 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
    NCT02442817 Schizophrenia Drug: Linagliptin University of Nevada, Reno|Augusta University Phase 4 2015-04-01 2016-05-19
    NCT02097342 Type 2 Diabetes Mellitus|Insulin Sensitivity/Resistance Drug: Linagliptin|Drug: Placebo|Drug: Voglibose Postgraduate Institute of Medical Education and Research Phase 4 2013-12-01 2014-04-06
    NCT02372630 Type 2 Diabetes Drug: Linagliptin|Drug: Placebo University at Buffalo|Kaleida Health Phase 4 2014-05-01 2016-05-10
    NCT02077309 Diabetes Mellitus Type 2 (T2DM),|Vascular Inflammation,|Plaque Morphology Drug: Linagliptin|Drug: Placebo RWTH Aachen University Phase 3 2014-08-01 2015-12-01
    NCT02106104 Type 2 Diabetes Drug: Linagliptin 5 mg QD (N=24)|Drug: Glimepiride 1 mg QD (N=24) VU University Medical Center Phase 4 2014-03-01 2016-05-16
    NCT01540487 Healthy Drug: linagliptin/metformin(high dose)|Drug: Linagliptin/metformin(low dose) Boehringer Ingelheim Phase 1 2012-02-01 2013-06-06
    NCT02350478 Type 2 Diabetes|Coronary Artery Disease Drug: Linagliptin|Drug: Placebo Medical University of Graz Phase 4 2013-07-01 2017-03-21
    NCT02376075 Arterial Hypertension|Albuminuria Drug: Linagliptin|Drug: Placebo ikfe-CRO GmbH|Ikfe GmbH|MLM Medical Labs M枚nchengladbach Phase 3 2013-01-01 2015-02-25
    NCT02212782 Healthy Drug: Linagliptin 5mg|Drug: DW1029M 1200mg and Linagliptin 5mg Dong Wha Pharmaceutical Co. Ltd. Phase 1 2014-09-01 2015-06-25
    NCT02015299 Type 2 Diabetes Mellitus Drug: Linagliptin|Drug: placebo dr. DJ Mulder|Boehringer Ingelheim|University Medical Center Groningen Phase 3 2014-03-01 2016-05-17
    NCT01617824 Type 2 Diabetes|Chronic Renal Failure Drug: Linagliptin|Drug: Placebo University of Padova Phase 4 2012-09-01 2014-12-18
    NCT02467478 Type 2 Diabetes|Impaired Renal Function Drug: Linagliptin|Drug: Placebo George Washington University|Boehringer Ingelheim Phase 4 2015-04-01 2017-03-17
    NCT03004612 Prediabetic State|Insulin Resistance Drug: Linagliptin + metformin|Other: Metformin Universidad de Guanajuato|Hospital Regional de Alta Especialidad del Bajio Phase 4 2015-12-01 2016-12-22
    NCT01943019 Schizophrenia Drug: Linagliptin Monash University|Pusat Perubatan Universiti Kebangsaan Malaysia Phase 1 2013-08-01 2016-09-23
    NCT02815644 Healthy Drug: empagliflozin/linagliptin FDC Boehringer Ingelheim Phase 1 2016-07-01 2017-02-07
    NCT02725502 Type 1 Diabetes Mellitus Drug: Linagliptin|Drug: Placebo Postgraduate Institute of Medical Education and Research 2013-07-01 2016-03-31
    NCT02857946 Healthy Drug: Prevaglip (linagliptin)|Drug: Trajenta (linagliptin) Genuine Research Center, Egypt|EVA pharma, Egypt Phase 1 2016-02-01 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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