Home > Gamma-secretase & Gamma-secretase & Gamma-secretase & > Avagacestat

Avagacestat

BMS-708163,BMS708163,BMS 708163

Avagacestat是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM，比作用于Notch选择性高193倍。

目录号
EY1072
EY1072
EY1072
纯度
99.25%
99.25%
99.25%
规格
1 mg
5 mg
10 mg
原价
540
1020
1950
售价
540
1020
1950
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
具体折扣请咨询客服

  • 生物活性

    BMS-708163(synonym: BMS 708163, BMS708163, Avagacestat) is a potent and orally active inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch protein. Oral dose of BMS-708163 markedly reduces Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    10 mg/kg (鼠) 或2.5 mg/kg (犬)每天口服饲喂

  • 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] Gillman KW, et al. Med Chem Lett, 2010, 1 (3), 120–124.
    [2] Crump CJ, et al. BMS-708,163 targets presenilin and lacks notch-sparing activity. Biochemistry. 2012 Sep 18;51(37):7209-11.

    分子式
    C20H17ClF4N4O4S    		 分子量
    520.88    		 CAS号
    1146699-66-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 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
    NCT00890890 Alzheimer's Disease Drug: Avagacestat|Drug: Placebo Bristol-Myers Squibb Phase 2 2009-05-01 2015-09-23
    NCT01039194 Alzheimer Disease Drug: galantamine|Drug: galantamine|Drug: BMS-708163 Bristol-Myers Squibb Phase 1 2010-01-01 2011-01-24
    NCT01042314 Alzheimer Disease Drug: Donepezil|Drug: BMS-708163 Bristol-Myers Squibb Phase 1 2010-01-01 2011-01-24
    NCT00860275 Alzheimer Disease Drug: BMS-708163|Drug: BMS-708163 + Ketoconazole|Drug: Ketoconazole|Drug: Fluconazole|Drug: BMS-708163 + Fluconazole Bristol-Myers Squibb Phase 1 2009-04-01 2011-01-24
    NCT01057030 Alzheimer Disease Drug: BMS-708163|Drug: Placebo Bristol-Myers Squibb Phase 1 2010-03-01 2011-01-24
    NCT01454115 Alzheimer's Disease Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: BMS-708163 (Gamma-Secretase Inhibitor)|Drug: Placebo matching BMS-708163|Drug: Placebo matching BMS-708163 Bristol-Myers Squibb Phase 1 2007-06-01 2011-11-18
    NCT01002079 Alzheimer Disease Drug: BMS-708163|Drug: Rifampin|Drug: Rifampin Bristol-Myers Squibb|PRA Health Sciences Phase 1 2010-08-01 2011-01-24
    NCT01079819 Alzheimer's Disease Drug: BMS-708163|Drug: BMS-708163|Drug: Placebo|Drug: Placebo Bristol-Myers Squibb Phase 1 2010-04-01 2011-02-04
    NCT00726726 Alzheimer Disease Drug: Interacting drugs - Cooperstown Cocktail (midazolam, warfarin, (+ vitamin K), caffeine, omeprazole and dextromethorphan)|Drug: BMS-708163|Drug: BMS-708163 + Cooperstown Cocktail Bristol-Myers Squibb Phase 1 2008-08-01 2008-11-04
    NCT00810147 Alzheimer's Disease Drug: BMS-708163|Drug: BMS-708163|Drug: BMS-708163|Drug: BMS-708163|Drug: Placebo Bristol-Myers Squibb Phase 2 2009-02-01 2015-09-23
    NCT00979316 Alzheimer Disease Drug: BMS-708163|Drug: BMS-708163|Drug: Placebo|Drug: Moxifloxacin Bristol-Myers Squibb Phase 1 2009-09-01 2011-01-06
    NCT00828646 Healthy Drug: BMS-708163|Drug: BMS-708163|Drug: BMS-708163|Drug: Placebo Bristol-Myers Squibb Phase 1 2008-10-01 2011-01-06
    NCT00901498 Alzheimer's Disease|Healthy Drug: BMS-708163|Drug: BMS-708163|Drug: BMS-708163|Drug: BMS-708163|Drug: BMS-708163 Bristol-Myers Squibb Phase 1 2009-05-01 2011-01-06

    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 ：
  • 收件地址 ：
  • 电话号码 ：
  • 单位名称 ：
  • 产品货号 ：
  • 产品规格 ：
  • 发票抬头以及单位税号 ：