Apremilast

阿普司特,CC-10004,CC10004,CC 10004,

Apremilast是一种口服生物有效的PDE4和TNF-α抑制剂,IC50分别为74 nM和77 nM。

目录号
EY1052
EY1052
EY1052
EY1052
EY1052
纯度
99.36%
99.36%
99.36%
99.36%
99.36%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
220
515
720
1020
1290
售价
220
515
720
1020
1290
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

    Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    5 mg/kg/day,分成每天两次的剂量口服处理

  • 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] Man HW, et al. J Med Chem, 2009,52(6), 1522-1524.

    分子式
    C22H24N2O7S
    分子量
    460.5
    CAS号
    608141-41-9
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    90 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
    NCT01634191 Healthy Volunteer Drug: Apremilast Celgene Corporation Phase 1 2012-02-01 2016-03-24
    NCT01634178 Healthy Volunteer Drug: Apremilast|Drug: Apremilast Celgene Corporation|Celgene Phase 1 2012-02-01 2012-07-05
    NCT02576678 Psoriasis Drug: Apremilast Celgene Phase 2 2015-10-01 2017-01-30
    NCT00521339 Psoriasis-Type Psoriasis|Plaque-Type Psoriasis Drug: Apremilast Celgene Corporation Phase 2 2007-08-01 2016-10-27
    NCT01925768 Psoriatic Arthritis Drug: Apremilast 30 mg|Drug: Placebo Celgene Corporation Phase 3 2013-09-01 2016-08-10
    NCT01561963 Healthy Drug: Apremilast|Drug: Rifampin Celgene Corporation Phase 1 2012-02-01 2016-11-21
    NCT00931242 Atopic Dermatitis|Allergic Contact Dermatitis Drug: Apremilast Tufts Medical Center|Celgene Corporation Phase 2 2009-06-01 2010-11-23
    NCT03082729 Psoriasis|Cardiovascular Diseases Drug: Apremilast University of Pennsylvania|Celgene Corporation|National Heart, Lung, and Blood Institute (NHLBI) Phase 4 2017-04-01 2017-03-10
    NCT01200264 Chronic Plaque Psoriasis Drug: apremilast Duke University Phase 2 2010-09-01 2014-07-14
    NCT01250548 Rheumatoid Arthritis Biological: apremilast|Other: Placebo Baylor Research Institute Phase 2 2010-05-01 2014-09-02
    NCT02775500 Psoriatic Arthritis|Psoriasis Drug: apremilast University of California, San Diego|Celgene|The Organization of Teratology Information Specialists 2014-11-01 2017-03-22
    NCT01074502 Acne Drug: apremilast University of North Carolina, Chapel Hill|Celgene Phase 2 2010-02-01 2017-02-01
    NCT02236988 Healthy Volunteers Drug: Apremilast Celgene Corporation Phase 1 2014-01-01 2016-03-24
    NCT02400749 Palmo-plantar Psoriasis Drug: Apremilast|Drug: Placebo Innovaderm Research Inc.|Celgene Phase 4 2015-05-01 2017-02-06
    NCT03000309 Plaque Psoriasis Drug: Apremilast Derm Research, PLLC|Celgene Phase 4 2016-12-29 2017-03-16
    NCT02307513 Behcet Syndrome Drug: Apremilast (CC-10004)|Drug: Placebo Celgene Corporation Phase 3 2014-12-01 2016-12-28
    NCT02641353 Healthy Volunteers Drug: Apremilast|Drug: Apremilast Oral Suspension Celgene Corporation Phase 1 2016-01-01 2016-03-25
    NCT01212770 Psoriatic Arthritis Drug: Apremilast 20mg|Drug: Apremilast 30mg|Drug: Placebo Celgene Phase 3 2010-09-01 2017-01-17
    NCT01232283 Plaque Psoriasis Drug: Apremilast|Drug: Placebo|Other: Topical or Phototherapy Therapy Celgene Phase 3 2010-11-01 2017-01-09
    NCT01307423 Psoriatic Arthritis Drug: Apremilast 20mg|Drug: Apremilast 30mg|Drug: Placebo Celgene Phase 3 2010-12-01 2017-01-17
    NCT00606450 Psoriasis Drug: CC-10004|Drug: CC-10004|Drug: Placebo Celgene Corporation|Celgene Phase 2 2006-04-01 2013-05-29
    NCT02425826 Parapsoriasis Drug: Apremilast|Drug: Placebo Celgene Corporation Phase 4 2015-04-01 2016-08-09

    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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