ML 224 是促甲状腺激素受体TSHR反激动剂,IC50值为2.3uM。
ML 224 是促甲状腺激素受体TSHR反激动剂,IC50值为2.3uM。
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] Neumann S, et al. A selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice. Endocrinology. 2014 Jan;155(1):310-4.
[2] Huang W, et al. Identification of Thyroid Stimulating Hormone Receptor Inverse Agonists. Probe Reports from the NIH Molecular Libraries Program.
分子式 C31H31N3O5 |
分子量 525.59 |
CAS号 1338824-21-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 10 mM |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00405574 | Prostate Cancer | Drug: ATN-224 | Attenuon|Prostate Cancer Clinical Trials Consortium | Phase 2 | 2006-11-01 | 2008-01-28 |
NCT02508805 | Vertebrogenic Radiculopathy L5, S1 | Drug: Neuromultivit|Drug: Voltaren|Drug: Sirdalud | Valeant Pharmaceuticals International, Inc.|Valeant Russia, LLC | Phase 3 | 2015-05-01 | 2015-09-27 |
NCT03072030 | Ebola Virus Disease|Prevention | Biological: GamEvac-Combi (vaccine)|Biological: Placebo | Gamaleya Research Institute of Epidemiology and Microbiology, Health Ministry of the Russian Federation|Military medical Academy named after S. M. Kirov | Phase 4 | 2017-06-01 | 2017-03-01 |
NCT02388672 | Blood Pressure | Dietary Supplement: decaffeinated coffee|Dietary Supplement: chlorogenic acid|Dietary Supplement: green coffee bean extract supplement|Dietary Supplement: placebo | University Hospital Tuebingen | 2015-03-01 | 2016-01-25 | |
NCT03063073 | Breast Cancer Female | Drug: Dexmedetomidine Injection [Precedex]|Drug: Bupivacaine | South Egypt Cancer Institute | Phase 3 | 2017-02-25 | 2017-02-23 |
NCT02819843 | Melanoma|Merkel Cell Carcinoma|Other Solid Tumors | Drug: TALIMOGENE LAHERPAREPVEC (TVEC)|Radiation: Hypofractionated Radiotherapy | Memorial Sloan Kettering Cancer Center|Amgen | Phase 2 | 2016-06-01 | 2017-02-22 |
NCT02663960 | Critical Illness|Kidney Replacement Disorder|Coagulation; Intravascular | Other: fixed citrate doses protocol|Other: adjusted citrate doses protocol | Peking Union Medical College Hospital | Phase 4 | 2015-08-01 | 2016-01-25 |
NCT02863211 | Cardiovascular Diseases|Vascular Stiffness | St. Boniface General Hospital Research Centre | 2015-09-01 | 2017-01-30 | ||
NCT00262522 | Human Immunodeficiency Virus Infections | Drug: lopinavir/ritonavir (LPV/r) (tablet or capsule) with nucleoside reverse transcriptase inhibitors (NRTIs)|Drug: lopinavir/ritonavir (LPV/r) (tablet or capsule) with nucleoside reverse transcriptase inhibitors (NRTIs)|Drug: lopinavir/ritonavir (LPV/r) (tablet or capsule) with nucleoside reverse transcriptase inhibitors (NRTIs)|Drug: lopinavir/ritonavir (LPV/r) (tablet or capsule) with nucleoside reverse transcriptase inhibitors (NRTIs) | Abbott | Phase 3 | 2005-11-01 | 2012-02-03 |
NCT00175877 | Rheumatoid Arthritis | Biological: Certolizumab Pegol | UCB Pharma | Phase 3 | 2005-06-01 | 2013-03-22 |
NCT01754480 | Parenchymous Tissue Surgical Bleeding | Biological: Fibrin Sealant Grifols|Device: Surgicel | Instituto Grifols, S.A.|Grifols Biologicals Inc. | Phase 3 | 2013-03-01 | 2016-12-16 |
NCT01571960 | HIV Infections | Biological: GEO-D03 DNA vaccine|Biological: MVA/HIV62B (MVA62B) vaccine|Biological: Placebo for GEO-D03 DNA|Biological: Placebo for MVA62B: | National Institute of Allergy and Infectious Diseases (NIAID)|GeoVax, Inc. | Phase 1 | 2012-04-01 | 2017-01-23 |
NCT01509781 | in Situ Breast Cancer|Invasive Breast Cancer | Procedure: Insertion of suction drain(s) following mastectomy|Procedure: Adaptive skin sutures. | National Institute of Oncology, Hungary | Phase 3 | 2011-09-01 | 2015-10-05 |
NCT00596752 | Peripheral Arterial Occlusive Disease | Drug: Alprostadil|Other: Placebo | UCB BIOSCIENCES GmbH|Aptiv Solutions|UCB Pharma | Phase 4 | 2004-03-01 | 2015-02-26 |
NCT01964989 | Influenza Virus | Biological: Adjuvanted Quadrivalent Subunit Influenza Virus Vaccine (aQIV)|Biological: Non-adjuvanted Trivalent Influenza Vaccine (TIV) / Quadrivalent Influenza Vaccine (QIV) | Seqirus|Novartis Vaccines | Phase 3 | 2013-11-01 | 2016-10-14 |
NCT02477839 | Epilepsy With Partial-onset Seizures | Drug: Lacosamide|Other: Placebo | UCB BIOSCIENCES, Inc.|UCB Pharma | Phase 3 | 2015-06-01 | 2017-02-02 |
NCT02326272 | Psoriasis|Plaque Psoriasis | Biological: Certolizumab Pegol|Other: Placebo | UCB Biopharma S.P.R.L.|Dermira, Inc.|UCB Pharma | Phase 3 | 2014-12-01 | 2017-03-09 |
NCT01521923 | Rheumatoid Arthritis | Biological: Certolizumab Pegol + Methotrexate (MTX)|Biological: Placebo + Methotrexate (MTX) | UCB Pharma | Phase 3 | 2012-01-01 | 2016-11-10 |
NCT01519791 | Rheumatoid Arthritis | Biological: Certolizumab Pegol|Other: Placebo|Biological: Methotrexate | UCB Pharma SA|UCB Pharma | Phase 3 | 2012-01-01 | 2016-01-20 |
NCT02743221 | Metastatic Colorectal Cancer | Drug: Trifluridine/tipiracil hydrochloride (S 95005)|Drug: Capecitabine|Drug: Bevacizumab|Drug: Bevacizumab | Institut de Recherches Internationales Servier|Servier | Phase 2 | 2016-04-01 | 2017-03-16 |
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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