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C34

TLR4-IN-C34,C 34,C-34

TLR4 inhibitor; attenuates TLR4 signaling in enterocytes and macrophages in vitro, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis (NEC). Also suppresses LPS signaling in human ileum displaying NEC ex-vivo. Displays no significant effects on signaling via TLR2 or TLR9.

目录号
EY2201
EY2201
EY2201
EY2201
纯度
99.22%
99.22%
99.22%
99.22%
规格
1 mg
5 mg
25 mg
50 mg
原价
270
680
1550
2550
售价
270
680
1550
2550
库存
现货
现货
现货
现货
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  • 生物活性

    Heparin, a highly sulfated glycosaminoglycan, is widely used as an injectable anticoagulant, and has the highest negative charge density of any known biological molecule.

  • 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 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。

  • 参考文献

    [1] Neal et al (2013) Discovery and validation of a new class of small molecule Toll-like receptor 4 (TLR4) inhibitors. PLoS One 8 e65779.
    [2] Axel Hollmann,et al. Conjugation of Cholesterol to HIV-1 Fusion Inhibitor C34 Increases Peptide-Membrane Interactions Potentiating Its Action. PLoS One. 2013; 8(4): e60302. Published online 2013 Apr 2. doi: 10.1371/journal.pone.0060302.
    [3] George J. Leslie,et al. Potent and Broad Inhibition of HIV-1 by a Peptide from the gp41 Heptad Repeat-2 Domain Conjugated to the CXCR4 Amino Terminus. PLoS Pathog. 2016 Nov; 12(11): e1005983. Published online 2016 Nov 17. doi: 10.1371/journal.ppat.1005983

    分子式
    C17H27NO9    		 分子量
    389.4    		 CAS号
    40592-88-9    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mM    		 Water
    50 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
    NCT03020524 Hiv Biological: Autologous CD4 T-Cells University of Pennsylvania Early Phase 1 2017-01-01 2017-01-11
    NCT02496182 Alveolitis Extrinsic Allergic|Pulmonary Fibrosis Drug: Placebo|Drug: Pirfenidone|Drug: Pirfenidone Grupo Medifarma, S. A. de C. V. Phase 2|Phase 3 2015-07-01 2015-07-13
    NCT00513110 Endotoxemia Genetic: AMPD1 polymorphism|Drug: Caffeine infusion|Drug: placebo Radboud University Phase 1 2007-08-01 2009-09-30
    NCT00548470 Schizophrenia|Tobocco Use Disorder|Nicotine Dependance Drug: Varenicline Nathan Kline Institute for Psychiatric Research|University of Illinois at Chicago Phase 4 2007-06-01 2012-05-17

    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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