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| CAS号: | 1146699-66-2 |
| 英文名称: | Avagacestat (BMS-708163) |
| 英文同义词: | BMS-708163;Avagacestat;BMS-708163 (Avagacestat);Avagacestat (BMS-708163);(R)-2-(4-Chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-phenylsulfonamido)-5,5,5-trifluoropen;(R)-2-(4-chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide;(2R)-2-(N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-4-chlorophenylsulfonamido)-5,5,5-trifluoropentanamide;(2R)-2-[N-[(4-Chlorophenyl)sulfonyl]-N-[2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl]amino]-5,5,5-trifluoropentanamide;(2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoro-pentanamide;(2R)-2-[N-[(4-Chlorophenyl)sulfonyl]-N-[2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl]amino]-5,5,5-trifluoropentanamide BMS-708163 |
| 中文名称: | Avagacestat (BMS-708163) |
| 中文同义词: | (2R)-2-[N-[(4-氯苯基)磺酰基]-N-[2-氟-4-(1,2,4-恶二唑-3-基)苄基]氨基]-5,5,5-三氟戊酰胺 |
| CBNumber: | CB32470907 |
| 分子式: | C20H17ClF4N4O4S |
| 分子量: | 520.8849928 |
| MOL File: | 1146699-66-2.mol |
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| Avagacestat (BMS-708163)化学性质 |
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Avagacestat (BMS-708163) 性质、用途与生产工艺 |
生物活性
Avagacestat (BMS-708163)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。Phase 2。
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体外研究
BMS-708163 抑制Notch 过程时显示出低选择性。
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体内研究
鼠和犬口服处理BMS-708163 明显且长期降低脑，血浆，脑脊液中的Aβ40 水平。BMS-708163作用于犬时，没有剂量限制影响(用3 mg/kg BMS-708163处理6个月内的犬)。
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特征
BMS-708163作用于Notch过程似乎比semagacestat (LY450139)效果要好，且所需量要少
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| Avagacestat (BMS-708163) 上下游产品信息 |
上游原料
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下游产品
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| 1146699-66-2, Avagacestat (BMS-708163) 相关搜索: |
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司马西特
ABT-737
DAPT
N1-[(7S)-6,7-二氢-6-氧代-5H-二苯并[B,D]氮杂卓-7-基]-2,2-二甲基-N3-(2,2,3,3,3-五氟丙基)丙二酰胺
(4S)-4-[2,4-二氟-5-(5-嘧啶基)苯基]-5,6-二氢-4-甲基-4H-1,3-噻嗪-2-胺
MK-0752
戊酰胺
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蛋白酶
信号转导通路激酶抑制剂
C20H17ClF4N4O4S
(2R)-2-[N-[(4-氯苯基)磺酰基]-N-[2-氟-4-(1,2,4-恶二唑-3-基)苄基]氨基]-5,5,5-三氟戊酰胺
1146699-66-2
(2R)-2-[N-[(4-Chlorophenyl)sulfonyl]-N-[2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl]amino]-5,5,5-trifluoropentanamide BMS-708163
(2R)-2-(N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-4-chlorophenylsulfonamido)-5,5,5-trifluoropentanamide
(R)-2-(4-Chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-phenylsulfonamido)-5,5,5-trifluoropen
Avagacestat (BMS-708163)
(2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoro-pentanamide
Avagacestat
BMS-708163 (Avagacestat)
(R)-2-(4-chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide
BMS-708163
(2R)-2-[N-[(4-Chlorophenyl)sulfonyl]-N-[2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl]amino]-5,5,5-trifluoropentanamide
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