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Halofuginone

Halofuginone is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.

目录号
EY2203
EY2203
EY2203
EY2203
纯度
98.56%
98.56%
98.56%
98.56%
规格
1 mg
5 mg
25 mg
50 mg
原价
540
1215
2800
4700
售价
540
1215
2800
4700
库存
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现货
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  • 生物活性

    Halofuginone is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.

  • 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] Tony L. H. Chu, et al. Halofuginone Synergistically Enhances Anti-Proliferation of Rapamycin in T Cells and Reduces Cytotoxicity of Cyclosporine in Cultured Renal Tubular Epithelial Cells. PLoS One. 2015; 10(12): e0144735.

    [2] Sun XH, et al. Halofuginone alleviates acute viral myocarditis in suckling BALB/c mice by inhibiting TGF-β1. Biochem Biophys Res Commun. 2016 Apr 29;473(2):558-64. 


    [2] Elizabeth F. Nelson,et al. Halofuginone down-regulates Smad3 expression and inhibits the TGFbeta-induced expression of fibrotic markers in human corneal fibroblasts. World J Gastroenterol. 2014 Oct 28; 20(40): 14778–14786. Published online 2014 Oct 28. doi: 10.3748/wjg.v20.i40.14778.
    [3] Sibo Huo, et al. Effect of halofuginone on the inhibition of proliferation and invasion of hepatocellular carcinoma HepG2 cell line. Int J Clin Exp Pathol. 2015; 8(12): 15863–15870. Published online 2015 Dec 1.

    分子式
    C16H17BrClN3O3    		 分子量
    414.68    		 CAS号
    55837-20-2    		 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

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00064142 AIDS-related Kaposi Sarcoma|Recurrent Kaposi Sarcoma Drug: halofuginone hydrobromide|Other: placebo|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 2 2003-05-01 2013-06-04
    NCT00027677 Unspecified Adult Solid Tumor, Protocol Specific Drug: halofuginone hydrobromide European Organisation for Research and Treatment of Cancer - EORTC Phase 1 2001-08-01 2012-07-23
    NCT02525302 Duchenne Muscular Dystrophy Drug: HT-100 Akashi Therapeutics Phase 2 2015-05-01 2016-02-03
    NCT01847573 Duchenne Muscular Dystrophy Drug: HT-100 Akashi Therapeutics Phase 1|Phase 2 2013-05-01 2016-02-03
    NCT01978366 Duchenne Muscular Dystrophy Drug: HT-100 Akashi Therapeutics Phase 2 2013-10-01 2016-02-03

    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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