Trichostatin A (TSA)是一种HDAC抑制剂,IC50为1.8 nM左右,HDAC8是HDAC家族中唯一不受TSA影响的成员。
Trichostatin A简称TSA,是一种常用的HDAC(histone deacetylase)抑制剂。Trichostatin A可以通透细胞,选择性抑制HDACs,但不抑制NAD依赖的SIRT系列的deacetylases。Trichostatin A抑制HDAC后可以导致histone乙酰化水平升高,一些基因的转录水平提高;也可以升高其它一些蛋白的乙酰化水平改变其活力或稳定性。Trichostatin A处理细胞后可以导致细胞周期抑制,目前被看作是一种潜在的抗癌药物。
1% DMSO+30% polyethylene glycol+1% Tween 80, pH 4
~10 μM
~5 mg/kg/day 皮下注射
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。
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[2] Futamura, M., et al., 1995. Trichostatin A inhibits both ras-induced neurite outgrowth of PC12 cells and morphological transformation of NIH3T3 cells. Oncogene. 10(6): 1119-23.
[3] Van Lint, C., et al., 1996. Transcriptional activation and chromatin remodeling of the HIV-1 promoter in response to histone acetylation. The EMBO journal. 15(5): 1112-20.
[4] Kawamura, Teruhisa., et al., 2005. Acetylation of GATA-4 is involved in the differentiation of embryonic stem cells into cardiac myocytes. The Journal of biological chemistry. 280(20): 19682-8.
[5] Takahashi, I., et al., 1996. Selective inhibition of IL-2 gene expression by trichostatin A, a potent inhibitor of mammalian histone deacetylase. The Journal of antibiotics. 49(5): 453-7.
[6] Pan, Lina., et al., 2007. Histone deacetylase inhibitor trichostatin a potentiates doxorubicin-induced apoptosis by up-regulating PTEN expression. Cancer. 109(8): 1676-88.
分子式 C17H22N2O3 |
分子量 302.37 |
CAS号 58880-19-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 20 mg/mL |
Water <1 mg/mL |
Ethanol 1 mg/mL |
体内溶解度
Rank | NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
1 | NCT00876447 | Overactive Bladder | Biological: Botulinum Toxin Type A 300U|Biological: Botulinum Toxin Type A 200U | Allergan | Phase 3 | 2009-01-01 | 2014-06-12 |
2 | NCT01157000 | Healthy | Drug: Canagliflozin | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. | Phase 1 | 2010-05-01 | 2014-04-07 |
4 | NCT01901198 | Healthy Volunteers | Biological: Human Serum Albumin/interferon alpha2a 300-1200 mcg single dose S.C.|Biological: Peginterferon 180 mcg single dose S.C. | Beijing Bio-Fortune Ltd. | Phase 1 | 2013-04-01 | 2014-11-14 |
5 | NCT00834912 | Healthy | Drug: Tramadol hydrochloride|Drug: Tramadol HCl|Drug: Tramadol HCl | Labopharm Inc. | Phase 1 | 2006-02-01 | 2012-04-25 |
6 | NCT03066401 | Dysmetabolic Syndrome|Hyperferritinemia|Obese | Procedure: echography | University Hospital, Lille | 2015-01-01 | 2017-02-27 | |
7 | NCT03066414 | Genetic Hemochromatosis | Procedure: echography | University Hospital, Lille | 2015-02-01 | 2017-02-27 | |
8 | NCT01703494 | Clostridium Difficile | Biological: Fecal Microbiota Transplantation|Biological: Sham Fecal Microbiota Transplantation | Colleen Kelly|The Miriam Hospital | Phase 2 | 2012-10-01 | 2015-09-29 |
9 | NCT00821834 | Stable Angina|Myocardial Infarction | Drug: clopidogrel (SR25990)|Drug: ticlopidine|Drug: Placebo | Sanofi | Phase 3 | 2008-12-01 | 2011-07-25 |
10 | NCT00284518 | Benign Prostatic Hyperplasia | Biological: botulinum toxin Type A|Drug: normal saline | Allergan | Phase 2 | 2005-12-01 | 2012-11-16 |
11 | NCT00276198 | Iron Deficiency Anemia|Infectious Diseases|Undernutrition | Dietary Supplement: Sprinkles|Dietary Supplement: Ferripel-3, Vitamins A&D drops | Soroka University Medical Center | Phase 3 | 2005-07-01 | 2008-04-15 |
13 | NCT01575054 | Muscle Spasticity | Biological: botulinum toxin Type A|Drug: Normal Saline | Allergan | Phase 3 | 2012-05-01 | 2016-08-22 |
14 | NCT01664702 | Childhood Obesity | Dietary Supplement: Dairy Products|Dietary Supplement: Dairy Servings | University of Kansas|Dairy Management Inc. | 2005-01-01 | 2012-08-13 | |
15 | NCT00559260 | Sedation for Non-Emergent Upper and/or Lower Endoscopy | Device: Passive monitoring with pulse-oximetry, NIBP and ECG | Ethicon Endo-Surgery | 2003-01-01 | 2008-09-12 | |
16 | NCT00631345 | Prediabetes|Obesity | Behavioral: Group-Based Lifestyle Intervention (Phases 1 and 2)|Other: Individual Education Program (All Phases)|Behavioral: Self-Directed Maintenance (Phase 3)|Behavioral: Extended Group Maintenance (Phase 3) | Wake Forest University Health Sciences|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) | 2007-08-01 | 2017-03-07 | |
17 | NCT02910635 | Abnormalities, Cardiovascular | Drug: Volanesorsen|Drug: Moxifloxacin|Drug: Placebo | Ionis Pharmaceuticals, Inc.|Akcea Therapeutics | Phase 1 | 2016-09-19 | 2017-03-07 |
18 | NCT01869465 | Schistosomiasis | Other: Pre-treatment snack|Behavioral: Education arm | Makerere University|University of Copenhagen | 2012-10-01 | 2013-06-01 | |
19 | NCT01080612 | Healthy | Drug: 330 mg pregabalin controlled release|Drug: 330 mg pregabalin controlled release|Drug: 330 mg pregabalin controlled release|Drug: 300 mg pregabalin immediate release | Pfizer | Phase 1 | 2010-04-01 | 2015-03-04 |
20 | NCT02098174 | Glomerular Filtration Rate|Acute Kidney Injury | Drug: MP-3180|Other: Iohexol comparator | MediBeacon | Phase 1 | 2013-11-01 | 2016-09-21 |
21 | NCT00439140 | Overactive Bladder | Biological: botulinum toxin Type A|Drug: Normal Saline (Placebo) | Allergan | Phase 3 | 2007-06-01 | 2013-12-09 |
22 | NCT00882739 | Acute Myocardial Infarction | Drug: Clopidogrel 300 mg|Drug: Clopidogrel 600 mg|Drug: Clopidogrel 900 mg | Ospedale San Donato | Phase 4 | 2009-04-01 | 2012-01-25 |
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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