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Sitagliptin phosphate monohydrate

磷酸西他列汀一水合物,MK-0431

Sitagliptin(MK 0431)是DPP4高效抑制剂，在Caco-2细胞中IC50值为19nM。

目录号
EY0985
EY0985
EY0985
纯度
99.25%
99.25%
99.25%
规格
100 mg
200 mg
500 mg
原价
400
550
800
售价
400
550
800
库存
现货
现货
现货
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  • 生物活性

    Sitagliptin phosphate (MK0431) is an orally active, potent and specific inhibitor of DPP-4, with IC50 of 19 nM in Caco-2 cell extracts. Sitagliptin phosphate, an orally active agent, potently inhibits CD26 (DPP-4) with an IC50 of 19 nM. Sitagliptin performs a direct, novel action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway in vitro.

  • 体外研究

  • 体内研究

    Saline

  • 激酶实验

  • 细胞实验

    100 μM

  • 动物实验

    ≤10 mg/kg 口服

  • 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] Thomas L et al. J Pharmacol Exp Ther. 2008; 325(1): 175-182.
    [2] Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73.[4]. Kim, S.J., et al., Inhibition of dipeptidyl p
    [3] Beconi, M.G., et al., Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35(4): p. 525-32.

    分子式
    C16H20F6N5O6P    		 分子量
    523.32    		 CAS号
    654671-77-9    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    50 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
    NCT01038648 Type 2 Diabetes Drug: Sitagliptin|Other: life style modification at base line India Diabetes Research Foundation & Dr. A. Ramachandran's Diabetes Hospitals Phase 3 2011-12-01 2015-12-29
    NCT01600703 Hyperlipidemia Drug: Sitagliptin|Drug: Placebo University Health Network, Toronto|Merck Frosst Canada Ltd. Phase 2|Phase 3 2012-07-01 2017-01-20
    NCT01159847 Type 1 Diabetes Drug: sitagliptin European Foundation for the Study of Diabetes|Chinese Medical Association|Eli Lilly and Company Phase 1|Phase 2 2010-01-01 2010-07-09
    NCT02900417 Type 2 Diabetes Drug: Sitagliptin Second Affiliated Hospital of Soochow University 2016-09-01 2016-09-08
    NCT02406950 Healthy Drug: Sitagliptin Kyunghee University Medical Center Phase 3 2015-02-01 2015-04-01
    NCT00659711 Type 2 Diabetes Drug: Januvia (Sitagliptin) 100 mg|Drug: Placebo Kaleida Health|Merck Sharp & Dohme Corp. 2008-03-01 2012-12-17
    NCT01095991 Type 2 Diabetes Mellitus Drug: AZD1656|Drug: Sitagliptin AstraZeneca Phase 1 2010-03-01 2010-06-30
    NCT00657280 Heart Failure, Congestive Drug: Sitagliptin Stanford University|Merck Sharp & Dohme Corp. Early Phase 1 2008-04-01 2014-12-04
    NCT00944450 Type 2 Diabetes Mellitus Drug: Sitagliptin phosphate anhydrous formulation|Drug: Comparator: sitagliptin phosphate monohydrate form Merck Sharp & Dohme Corp. Phase 1 2004-08-01 2015-08-18
    NCT02294084 Neoplasms, Adipose Tissue Drug: Sitagliptin|Drug: placebo IngridJazet|Merck Sharp & Dohme Corp.|Leiden University Medical Center Phase 4 2014-03-01 2016-03-24
    NCT00978796 Type 1 Diabetes Drug: Sitagliptin|Drug: Sugar Pill University of Colorado Denver School of Medicine Barbara Davis Center Phase 4 2009-09-01 2010-03-29
    NCT01686932 Diabetes Mellitus Type 2 Drug: Vildagliptin|Drug: Sitagliptin Novartis Pharmaceuticals|Novartis Phase 4 2012-11-01 2016-02-02
    NCT00730275 Type 2 Diabetes Drug: Sitagliptin phosphate|Drug: Comparator: matching placebo Merck Sharp & Dohme Corp. Phase 1 2008-07-01 2015-08-07
    NCT01720264 Acute Myeloid Leukemia|Acute Lymphoid Leukemia|Hematopoetic Myelodysplasia|Leukemia, Myelogenous, Chronic|Lymphoma, Non-Hodgkin Drug: Sitagliptin Sherif S. Farag|National Heart, Lung, and Blood Institute (NHLBI)|Indiana University Phase 2 2012-11-01 2016-06-16
    NCT02536248 Type 2 Diabetes Mellitus Drug: Sitagliptin|Drug: Placebo Laval University|Merck Sharp & Dohme Corp. Phase 3 2015-08-01 2016-09-07
    NCT01034111 Type 2 Diabetes Drug: Sitagliptin phosphate|Drug: Metformin Merck Sharp & Dohme Corp. Phase 3 2010-03-01 2015-08-07
    NCT01334229 Type 2 Diabetes Mellitus Drug: Sitagliptin|Drug: Placebo Laval University|Merck Sharp & Dohme Corp. Phase 3 2011-04-01 2016-03-07
    NCT00969566 Diabetes Drug: sitagliptin, metformin Seoul National University Bundang Hospital Phase 4 2009-01-01 2012-01-05
    NCT00696826 Liver Insufficiency Drug: sitagliptin phosphate Merck Sharp & Dohme Corp. Phase 1 2004-04-01 2015-08-18
    NCT00686634 Type 2 Diabetes Mellitus Drug: Sitagliptin Charles Drew University of Medicine and Science|National Center for Research Resources (NCRR) Phase 4 2008-01-01 2014-11-25
    NCT01512797 Type 2 Diabetes Mellitus Drug: Sitagliptin phosphate|Other: Placebo Blandine Laferrere|Merck Sharp & Dohme Corp.|Columbia University 2012-07-01 2016-10-11

    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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