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BEGACESTAT

BEGACESTAT, 769169-27-9, 结构式
BEGACESTAT
CAS号:
769169-27-9
英文名:
Begacestat
英文别名:
GSI-953;Begacestat;Begacestat(GSI-953);GSI-953 DISCONTINUED;Begacestat (Synonyms: GSI-953);5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxyMethyl)-2-(trifluoroMethyl)propyl]-2-thiophenesulfonaMide;2-Thiophenesulfonamide, 5-chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-;5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2- (trifluoromethyl)propyl] thiophene-2-sulfonamide;(2S)-S-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-hydroxy-N-Methyl-3-(trifluoroMethyl)butane-2-sulfonaMido
中文名:
BEGACESTAT
中文别名:
贝加塞特;化合物 T14525;5-氯-N-[(1S)-3,3,3-三氟-1-(羟基甲基)-2-(三氟甲基)丙基]-2-噻吩磺酰胺
CBNumber:
CB72535664
分子式:
C9H8ClF6NO3S2
分子量:
391.74
MOL File:
769169-27-9.mol

BEGACESTAT化学性质

熔点:
153-155°C
沸点:
355℃
密度:
1.642
闪点:
169℃
储存条件:
2-8°C
溶解度:
DMSO: ≥15mg/mL
形态:
powder
酸度系数(pKa):
8.16±0.50(Predicted)
颜色:
white to tan
安全信息
WGK Germany: 3

BEGACESTAT性质、用途与生产工艺

生物活性

Begacestat (GSI-953) 是淀粉样前体蛋白 γ 分泌酶 (gamma-secretase) 的选择性噻吩磺酰胺抑制剂 (IC50Aβ40=15 nM),有潜力用于阿尔兹海默症的研究。

靶点

IC50: 15 nM (Aβ 40 ).

体内研究

Begacestat (5 mg/kg, p.o. in mice) treatment for 4 h significantly reduces the Aβ 40 and Aβ 42 in brain (37% lowering of brain Aβ 40 and 25% lowering of Aβ 40 observed).
Begacestat (GSI-953: 0, 2.5, 5, or 10 mg/kg, oral gavage, 3 h) results in a dose-dependent reversal of contextual fear conditioning deficits when compound is orally administered 3 h before training. Significant deficits are observed after treatment with 2.5 mg/kg Begacestat, and there is some reversal of this at 5 mg/kg and full reversal at 10 mg/kg compared with vehicle-dosed Tg2576 mice.
A dosage-related trend of slightly lower percentages of SP CD4+ cells in males at all dosages (SP CD4+ cells=~11% in controls compared with ~7% to ~9% in Begacestat-dosed animals) and females at 2000 mg/kg/day (SP CD4+ cells=~10% in controls compared with ~8% in Begacestat-dosed animals) is observed.

Animal Model: Tg2576 mice
Dosage: 0, 2.5, 5, or 10 mg/kg
Administration: Oral gavage for two consecutive days
Result: Resulted in a dose-dependent reversal of contextual fear conditioning deficits when compound is orally administered 3 h before training.
Animal Model: Sprague-Dawley rats
Dosage: 0, 200, 600, or 2000 mg/kg/day for 10 (5 males/group and 5 females at 600 mg/kg/day) or 28 (10/sex/group) consecutive days
Administration: P.O. for 10 (5 males/group and 5 females at 600 mg/kg/day) or 28 (10/sex/group) consecutive days.
Result: A dosage-related trend of slightly lower percentages of SP CD4+ cells in males at all dosages and females at 2000 mg/kg/day was observed.

BEGACESTAT 上下游产品信息

上游原料

下游产品

BEGACESTAT 试剂级价格

更新日期产品编号产品名称CAS编号包装价格
2024/01/25HY-14175BEGACESTAT
Begacestat
769169-27-91mg800元
2024/01/25HY-14175BEGACESTAT
Begacestat
769169-27-910mM * 1mLin DMSO1100元

BEGACESTAT 生产厂家

全球有 53家供应商   BEGACESTAT国内生产厂家
供应商联系电话电子邮件国家产品数优势度
北京百灵威科技有限公司 010-82848833 400-666-7788 jkinfo@jkchemical.com 中国 96815 76
凯试(上海)科技有限公司 021-50135380 shchemsky@sina.com 中国 15421 60
上海偕腾生物科技有限公司 +86-021-58975553 sales@cooperpharm.com 中国 1210 56
深圳振强生物技术有限公司 0755-66853366 15920483169 sales@chem-strong.com 中国 17944 56
上海一飞生物科技有限公司 021-65675885 18964387627 info@efebio.com 中国 9709 58
苏州贝昶生物科技有限公司 +86-18017644823 sales@betterbiochem.com 中国 325 58
深圳聚合生化科技有限公司 +86-400-002-6226 13028896684 sales@rrkchem.com 中国 55477 58
爱诗伦生物科技(上海)有限公司 021-50676523 18019098996 info@acelybio.com 中国 3967 58
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 marketing@targetmol.com 美国 19892 58
上海源溪生物科技有限公司 021-58447131 13564518121 sales@dcchemicals.com 中国 9414 58
上海炎泽化工有限公司 13773155751; 19962611955 260924549@qq.com 中国 8506 58
ChemeGen 中国 18818260767 sales@chemegen.com 中国 11289 58
MedBio脉铂医药 021-69568360 18916172912 order@med-bio.cn 中国 8141 58
安耐吉化学&3A(安徽泽升科技有限公司) 021-58432009 400-005-6266 marketing@energy-chemical.com 中国 44941 58
成都超九八生物科技有限公司 13348960310 13348960310 3003867561@qq.com 中国 9945 58
常州孚睿斯生物科技有限公司 0519-85524369 3477467573@qq.com 中国 8618 58
天津普西唐生物医药科技有限公司 010-60605840 15801484223 psaitong@jm-bio.com 中国 29834 58
TargetMol中国(陶术生物) 4008200310 marketing@tsbiochem.com 中国 24131 58
南通全益生物科技有限公司 0513-66337626 18051384581 sales@chemhifuture.com 中国 3913 58
上海炎泽化工有限公司 021-13621551597 19901447308 260924549@qq.com 中国 6456 58
杭州摩库生物医药科技有限公司 +86-057181025280; +8617767106207 sales@molcore.com 中国 49739 58
ApexBio技术 sales@apexbt.com 美国 6254 58
 

769169-27-9, BEGACESTAT 相关搜索:

  • Sulfur & Selenium Compounds
  • Pharmaceuticals
  • Pfizer Compounds
  • Intermediates & Fine Chemicals
  • Inhibitors
  • Heterocycles
  • C9H8ClF6NO3S2
  • 化合物 T14525
  • 贝加塞特
  • 5-氯-N-[(1S)-3,3,3-三氟-1-(羟基甲基)-2-(三氟甲基)丙基]-2-噻吩磺酰胺
  • 769169-27-9
  • GSI-953 DISCONTINUED
  • Begacestat (Synonyms: GSI-953)
  • 2-Thiophenesulfonamide, 5-chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-
  • 5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2- (trifluoromethyl)propyl] thiophene-2-sulfonamide
  • (2S)-S-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-hydroxy-N-Methyl-3-(trifluoroMethyl)butane-2-sulfonaMido
  • 5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxyMethyl)-2-(trifluoroMethyl)propyl]-2-thiophenesulfonaMide
  • GSI-953
  • Begacestat(GSI-953)
  • Begacestat
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