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Laquinimod

拉喹莫德,ABR-215062,LAQ,ABR 215062,ABR215062,

Laquinimod是一种中枢神经系统（CNS）免疫调节剂。0.1-1 μM Laquinimod 处理不影响外周血单核细胞(PBMC)活性。通过在健康对象和复发缓解型多发性硬化症(RRMS)患者的PBMC中进行大规模基因表达芯片分析 ,显示 Laquinimod 抑制与抗原呈递及相应炎症通路相关的基因表达。Laquinimod作用于CD14+ 和 CD4+细胞，诱导Th2反应激活，作用于CD8+细胞，抑制增殖。

目录号
EY0325
EY0325
EY0325
纯度
99.51%
99.51%
99.51%
规格
2 mg
10 mg
50 mg
原价
560
920
3600
售价
560
920
3600
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Laquinimod is a potent immunomodulator. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    溶于PBS, ~1 μM

  • 动物实验

    0.16, 1.6 和 16 mg/kg/day每天皮下注射

  • 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 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] Kramann N,et al. Laquinimod prevents cuprizone-induced demyelination independent of Toll-like receptor signaling. Neurol Neuroimmunol Neuroinflamm. 2016 May 17;3(3):e233. doi: 10.1212/NXI.0000000000000233.
    [2] Ehrnhoefer DE,et al. Laquinimod decreases Bax expression and reduces caspase-6 activation in neurons. Exp Neurol. 2016 Sep;283(Pt A):121-8. doi: 10.1016/j.expneurol.2016.06.008.
    [3] Dobson L,et al. Laquinimod dampens hyperactive cytokine production in Huntington's disease patient myeloid cells. J Neurochem. 2016 Jun;137(5):782-94. doi: 10.1111/jnc.13553.

    分子式
    C19H17ClN2O3    		 分子量
    356.8    		 CAS号
    248281-84-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    ≥60 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    1 mg/mL

    体内溶解度

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

    NCT01047319 Relapsing Multiple Sclerosis Drug: Laquinimod Teva Pharmaceutical Industries Phase 3 2010-04-01 2016-12-01
    NCT01085084 Lupus Arthritis Drug: Laquinimod|Drug: Laquinimod|Other: Placebo Teva Pharmaceutical Industries Phase 2 2010-07-01 2016-07-18
    NCT00737932 Crohn's Disease Drug: Laquinimod|Other: placebo Teva Pharmaceutical Industries Phase 2 2010-05-01 2015-03-19
    NCT02085863 Pharmacokinetics|Pharmacodynamics Drug: laquinimod|Drug: Placebo Teva Pharmaceutical Industries Phase 1 2014-02-01 2015-01-26
    NCT00509145 Multiple Sclerosis Drug: Laquinimod|Other: Placebo Teva Pharmaceutical Industries Phase 3 2007-12-01 2012-02-16
    NCT00349193 Relapsing Remitting Multiple Sclerosis Drug: laquinimod 0.3|Drug: laquinimod 0.6|Other: Placebo Teva Pharmaceutical Industries Phase 2 2005-03-01 2011-04-07
    NCT01085097 Lupus Nephritis Drug: laquinimod|Drug: Mycophenolate Mofetil|Drug: prednisolone/prednisone|Drug: Placebo Teva Pharmaceutical Industries Phase 2 2010-07-01 2016-07-20
    NCT02284568 Primary Progressive Multiple Sclerosis Drug: Laquinimod|Drug: Placebo Teva Pharmaceutical Industries Phase 2 2015-01-01 2016-12-01
    NCT00988052 Relapsing Multiple Sclerosis (RMS) Drug: Laquinimod Teva Pharmaceutical Industries Phase 3 2009-11-01 2016-12-01
    NCT00745615 Relapsing Remitting Multiple Sclerosis Drug: laquinimod Teva Pharmaceutical Industries Phase 2 2006-12-01 2016-12-01
    NCT02215616 Huntington's Disease Drug: Laquinimod|Drug: Placebo Teva Branded Pharmaceutical Products, R&D Inc.|Teva Pharmaceutical Industries Phase 2 2014-11-01 2017-03-21
    NCT01975298 Relapsing Remitting Multiple Sclerosis Drug: Laquinimod|Drug: Avonex庐 Teva Pharmaceutical Industries Phase 3 2014-01-01 2014-03-03
    NCT01707992 Multiple Sclerosis (MS) Drug: Laquinimod 0.6 mg|Drug: Matching Placebo|Drug: Laquinimod 1.2 mg Teva Pharmaceutical Industries Phase 3 2013-02-01 2016-12-01
    NCT00605215 Multiple Sclerosis Drug: laquinimod|Drug: placebo|Drug: Interferon 尾-1a (Avonex庐) Teva Pharmaceutical Industries Phase 3 2008-04-01 2013-08-16
    NCT01404117 Relapsing Multiple Sclerosis Drug: Laquinimod 0.6|Drug: Laquinimod 1.2|Other: Glatiramer Acetate or interferon-beta+ Placebo Teva Pharmaceutical Industries Phase 2 2012-03-01 2013-08-26

    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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