769169-27-9
769169-27-9 structure
- Name: Begacestat
- Chemical Name: 5-chloro-N-[(2S)-4,4,4-trifluoro-1-hydroxy-3-(trifluoromethyl)butan-2-yl]thiophene-2-sulfonamide
- CAS Number: 769169-27-9
- Molecular Formula: C9H8ClF6NO3S2
- Molecular Weight: 391.73800
- Catalog: Research Areas Neurological Disease
- Create Date: 2016-05-03 12:16:31
- Modify Date: 2024-01-09 14:16:27
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Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC50Aβ40=15 nM) for the treatment of Alzheimer's disease[1].
| Name | 5-chloro-N-[(2S)-4,4,4-trifluoro-1-hydroxy-3-(trifluoromethyl)butan-2-yl]thiophene-2-sulfonamide |
|---|---|
| Synonyms |
GSI-953
UNII-3666C56BBU Begacestat |
| Description | Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC50Aβ40=15 nM) for the treatment of Alzheimer's disease[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 15 nM (Aβ40)[1]. |
| In Vivo | Begacestat (5 mg/kg, p.o. in mice) treatment for 4 h significantly reduces the Aβ40 and Aβ42 in brain (37% lowering of brain Aβ40 and 25% lowering of Aβ40 observed)[1]. 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[2]. 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[2]. Animal Model: Tg2576 mice[2] 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[2] 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. |
| References |
| Molecular Formula | C9H8ClF6NO3S2 |
|---|---|
| Molecular Weight | 391.73800 |
| Exact Mass | 390.95400 |
| PSA | 103.02000 |
| LogP | 4.25320 |
| RIDADR | NONH for all modes of transport |
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