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ISO 1

ISO-1,ISO1,MIF Antagonist

ISO 1 is an inhibitor of MIF d-dopachrome tautomerase activity with an IC50 of about 7 uM.

目录号
EY2040
EY2040
EY2040
纯度
99.24%
99.24%
99.24%
规格
5 mg
10 mg
50 mg
原价
712
1120
3430
售价
712
1120
3430
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    ISO 1 is a cell permeable and orally bioavailable macrophage migration inhibitory factor (MIF) inhibitor
    (IC50 = 7 μM), ISO 1 inhibits MIF tautomerase activity in vitro and in vivo. Protective against mouse models
    of streptozotocin-induced diabetes mellitus. ISO 1 blocks anti-inflammatory response following LPS exposure
    and increases survival. Also it inhibits airway remodeling in a mouse model of chronic asthma.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 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 AKm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] Al-Abed Y, et al. ISO-1 binding to the tautomerase active site of MIF inhibits its pro-inflammatory activity and increases survival in severe sepsis. J Biol Chem. 2005 Nov 4;280(44):36541-4.
    [2] Nothnick WB, et al. Inhibition of macrophage migration inhibitory factor reduces endometriotic implant size in mice with experimentally induced disease. J Endometr. 2011 Sep 30;3(3):135-142.
    [3] Lubetsky JB, et al. The tautomerase active site of macrophage migration inhibitory factor is a potential target for discovery of novel anti-inflammatory agents. J Biol Chem. 2002 Jul 12;277(28):24976-82.

    分子式
    C12H13NO4
    分子量
    235.24
    CAS号
    478336-92-4
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    40 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
    NCT02284919 Breast Cancer|Breast Neoplasm Drug: [18F]ISO-1 University of Pennsylvania Phase 1 2014-11-01 2016-08-29
    NCT00968656 Breast Cancer|Head and Neck Cancer|Diffuse Large B-cell Lymphoma Radiation: PET/CT|Other: Laboratory Testing|Other: Safety Testing|Other: Immunohistochemistry staining|Drug: F-18-ISO Washington University School of Medicine|Isotrace Technologies Phase 1 2009-01-01 2014-12-08
    NCT03057743 METASTATIC BREAST CANCER Device: Positron emission tomography (PET/CT) imaging|Device: radiotracer [18F]ISO-1 Abramson Cancer Center of the University of Pennsylvania 2016-04-05 2017-02-16
    NCT02762110 Breast Cancer Drug: N-(4-(6,7-dimethoxy-3,-4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-[18F]- fluoroethoxy)-5-methylbenzamide (18F-3c) ([18F]ISO-1)|Radiation: Positron emission tomography (PET/CT) imaging Abramson Cancer Center of the University of Pennsylvania Phase 1 2014-10-01 2016-05-09
    NCT02204202 Lung Disease Drug: [18F]FDG|Drug: [18F]ISO-1 Washington University School of Medicine|National Heart, Lung, and Blood Institute (NHLBI) Phase 1 2014-02-01 2016-11-02
    NCT01478022 Duchenne Muscular Dystrophy (DMD) Drug: Isosorbide Dinitrate|Drug: Ibuprofen|Other: Ibuprofen and Isosorbide Dinitrate combination Parent Project, Italy Phase 1 2011-10-01 2011-11-22
    NCT02249650 Metastatic Colorectal Cancer Drug: TSB-9-W1 Taiwan Sunpan Biotechnology Development Co., Ltd. Phase 1 2016-05-01 2016-04-22
    NCT02503891 Osteoarthritis|Avascular Necrosis|Rheumatoid Arthritis|Congenital Dysplasia of the Hip|Ankylosing Spondylitis|Post-traumatic; Arthrosis|Injury of Hip Device: MP-1 Polymer on Ceramic Articulation system M.M.A Tech Ltd. 2015-09-01 2015-07-18
    NCT01379287 Solid Tumors Drug: Iso-Fludelone Memorial Sloan Kettering Cancer Center|University of Pittsburgh|Bristol-Myers Squibb Phase 1 2011-06-01 2016-07-12
    NCT00655603 Type 2 Diabetes Mellitus Other: Infusion of native hormones from the pancreas and gut (GLP-1) University Hospital, Gentofte, Copenhagen|University of Copenhagen|Hvidovre University Hospital|Glostrup University Hospital, Copenhagen 2008-03-01 2009-04-03
    NCT02977234 Hydrosalpinx|Infertility, Female Drug: Isoamyl 2-Cyanoacrylate Ain Shams University Phase 1|Phase 2 2016-10-01 2016-11-29
    NCT00042471 Diabetes Mellitus, Type 1|Diabetes Mellitus, Type 2 Drug: Pramlintide acetate AstraZeneca Phase 2 2002-06-01 2015-09-22
    NCT02753387 Bacterial Infection Drug: Chlorhexidine|Device: NaCl 0.9 % Rennes University Hospital Phase 3 2016-05-01 2016-05-24
    NCT02833207 Obesity Drug: Drug Trial 1 (EDD)|Drug: Drug Trial 2 (ROV) University of Wisconsin, Madison Phase 1 2011-07-01 2016-08-26
    NCT03050125 Contact Lens Related Dry Eye Device: Hypo-osmolar drop 1|Device: Hypo-osmolar drop 2|Device: Iso-osmolar drop Centre for Contact Lens Research|Coopervision, Inc.|University of Waterloo 2017-02-07 2017-02-09
    NCT00107107 Diabetes Mellitus, Type 1 Drug: pramlintide acetate AstraZeneca Phase 3 2002-11-01 2015-09-22
    NCT00108004 Type 1 Diabetes Mellitus|Type 2 Diabetes Mellitus Drug: pramlintide acetate AstraZeneca Phase 3 2003-04-01 2015-05-20
    NCT01714635 Cataract Device: Tecnis Multifocal Intraocular Lens|Device: Monofocal Intraocular Lens Abbott Medical Optics Phase 1 2012-11-01 2015-02-26
    NCT02479035 Insulin Resistant Dietary Supplement: Red raspberry meal 1|Dietary Supplement: Red raspberry meal 2|Dietary Supplement: Control meal Institute for Food Safety and Health, United States 2015-06-01 2017-02-06
    NCT00195572 Gastric Cancer Drug: Isovorin|Drug: TS-1 Wyeth is now a wholly owned subsidiary of Pfizer Phase 3 2002-05-01 2009-08-12

    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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