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