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Dorsomorphin 2HCl

BML-275,Compound C

Dorsomorphin 2HCl是一种有效的,可逆的AMPK选择性抑制剂,Ki为109 nM,对ZAPK, SYK, PKCθ, PKA和JAK3没有显著的抑制作用。

目录号
EY1667
EY1667
EY1667
EY1667
EY1667
纯度
99.19%
99.19%
99.19%
99.19%
99.19%
规格
5 mg
10 mg
20 mg
50 mg
100 mg
原价
500
800
1200
3205
5260
售价
500
800
1200
3205
5260
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Dorsomorphin 2HCl是一种有效的,可逆的AMPK选择性抑制剂,Ki为109 nM,对一些结构相关的激酶,包括ZAPK, SYK, PKCθ, PKA和JAK3没有显著的抑制作用。同时抑制了BMP一型受体作用。

  • 体外研究

  • 体内研究

    1% DMSO+30% polyethylene glycol+1% Tween 80

  • 激酶实验

  • 细胞实验

  • 动物实验

    ~10 mg/kg 静脉注射

  • 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] Zhou G, et al. J Clin Invest. 2001, 108(8), 1167-1174.
    [2] Vucicevic et al (2011) Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway. Autophagy 7 40.
    [3] Diekmann et al (2015) A reliable and efficient protocol for human pluripotent stem cell differentiation into the definitive endoderm based on dispersed single cells. Stem Cells Dev. 24 190.
    [4] Hao et al (2008) Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells. PLoS ONE 3 2904.

    分子式
    C24H25N5O.2HCl
    分子量
    472.41
    CAS号
    1219168-18-9
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    20 mM
    Water
    100 mM
    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
    NCT01251562 Solid Tumors Drug: Sterile Compound c31510 for Injection Berg, LLC Phase 1 2011-01-01 2014-05-15
    NCT01607476 Alzheimer's Disease Drug: C11 PiB|Drug: F18 Flutametamol Mayo Clinic Phase 2 2012-07-01 2016-11-08
    NCT00811122 Alzheimer's Disease Radiation: 11C-PIB PET Scan|Radiation: FDG-PET Scan University of Utah Early Phase 1 2009-11-01 2016-08-09
    NCT01032031 Skin Cancer Dietary Supplement: Green tea + vitamin C high dose|Dietary Supplement: Placebo capsule University of Manchester|University of Leeds|University of Bradford 2009-03-01 2016-03-07
    NCT02689843 Polycystic Ovary Syndrome Drug: Cyproterone compound + Spironolactone|Drug: Metformin|Drug: Pioglitazone Shiraz University of Medical Sciences Early Phase 1 2016-03-01 2016-08-02
    NCT02093169 Healthy Men Drug: Part A: Lu AF35700|Drug: Part B: Lu AF35700 H. Lundbeck A/S Phase 1 2014-02-01 2014-09-22
    NCT00704990 Attention Deficit Hyperactivity Disorder Dietary Supplement: Zinc, Magnesium, Vitamin B6, Vitamin C (Compound Natural Health Product for ADHD) Kieran Cooley|The Canadian College of Naturopathic Medicine|University of Toronto|Centre for Addiction and Mental Health Phase 2|Phase 3 2008-09-01 2015-10-15
    NCT00866853 Hepatitis C|Viruses Drug: TMC435 Tibotec Pharmaceuticals, Ireland Phase 1 2009-03-01 2010-04-26
    NCT00175695 Pre-eclampsia Drug: Recombinant human activated protein C or drotrecogin alpha University of British Columbia Phase 2 2004-12-01 2011-02-03
    NCT00908414 HIV Infections Drug: TMC589337 40 mg|Drug: TMC589337 100 mg|Drug: TMC589337 200 mg|Drug: TMC589337 400 mg|Drug: TMC589354 40 mg|Drug: TMC589354 100 mg|Drug: TMC589354 200 mg|Drug: TMC589354 400 mg|Drug: TMC589337 AA mg|Drug: TMC589354 BB mg|Drug: TMC589337 CC mg|Drug: TMC589354 DD mg|Drug: TMC589337 EE mg|Drug: TMC589354 YY mg|Drug: TMC310911 300 mg|Drug: TMC310911 600 mg|Drug: Placebo Tibotec Pharmaceuticals, Ireland Phase 1 2009-05-01 2016-10-27
    NCT02410525 Healthy Drug: [11C]PF-06427878|Drug: PF-06427878 10 mg|Drug: PF-06427878 600 mg Pfizer Phase 1 2015-05-01 2015-10-27
    NCT01063946 Neoplasms, Malignant Drug: Ombrabulin (AVE8062) Sanofi Phase 1 2010-01-01 2011-12-20
    NCT01022229 Attention Deficit Hyperactivity Disorder Dietary Supplement: Compound Natural Health Product|Dietary Supplement: Placebo The Canadian College of Naturopathic Medicine|Health Canada|Centre for Addiction and Mental Health|SickKids Foundation Phase 3 2013-11-01 2016-01-27
    NCT02120664 Alzheimer's Disease Drug: Florbetapir (18F)|Drug: 11C-PiB Avid Radiopharmaceuticals Phase 1 2014-04-01 2017-01-20
    NCT02564562 Healthy Drug: [14C] PF-06463922 Pfizer Phase 1 2015-10-01 2015-12-03
    NCT02240290 N/A, as Healthy Volunteers Drug: tozadenant tablet|Drug: C14-tozadenant capsule Biotie Therapies Inc.|PRA Health Sciences|Tandem Labs|Xceleron Inc Phase 1 2013-09-01 2016-01-13
    NCT02448004 Healthy Drug: JNJ-63623872 Janssen Cilag N.V./S.A. Phase 1 2015-05-01 2016-07-07
    NCT02211885 Healthy Drug: 14C-BIRB 796 BS Boehringer Ingelheim Phase 1 2002-10-01 2014-08-07
    NCT01961505 Rheumatoid Arthritis Drug: Compound tripterygium gel|Drug: Placebo Guang'anmen Hospital of China Academy of Chinese Medical Sciences Phase 2|Phase 3 2011-10-01 2013-10-09
    NCT01723553 Atypical Alzheimers Disease|Logopenic Variant of Primary Progressive Aphasia (LPA)|Posterior Cortical Atrophy (PCA) Drug: C-11 PiB Mayo Clinic Phase 1 2012-11-01 2015-12-18

    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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