BMS 299897 ≥98%(HPLC)

BMS 299897

源叶(MedMol)
S84797
290315-45-6
C24H21ClF3NO4S
511.94
2-[(1R)-1-[[(4-氯苯基)磺酰基](2,5-二氟苯基)氨基]乙基]-5-氟苯丁酸;Benzenebutanoic acid, 2-[(1R)-1-[[(4-chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl]-5-fluoro-; 4-[2-[(1R)-1-(N-(4-chlorophenyl)sulfonyl-2,5-diflu
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) S84797-5mg ≥98%(HPLC) ¥621.00元 3 - - -
源叶(MedMol) S84797-10mg ≥98%(HPLC) ¥1181.00元 4 - - -
源叶(MedMol) S84797-25mg ≥98%(HPLC) ¥2700.00元 2 - - -
源叶(MedMol) S84797-50mg ≥98%(HPLC) ¥4463.00元 1 - - -
源叶(MedMol) S84797-100mg ≥98%(HPLC) ¥8800.00元 1 - - -
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产品介绍

BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
产品描述: BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
靶点: IC50: 7 nM (Aβ, in HEK293 cells);BetaAmyloid;Gamma-secretase
体内研究: BMS-299897 shows dose- and time-dependent reductions of amyloid β-peptide (Aβ) in brain, cerebrospinal fluid (CSF), and plasma in young transgenic mice, with a correlation between brain and CSF Aβ levels. BMS-299897 reduces both brain and plasma Aβ1-40 in APP-YAC mice and increases brain concentrations of APPcarboxy-terminal fragments, consistent with γ-secretase inhibition. BMS-299897, attenuates this Aβ25-35-induced Aβ1-42 seeding and toxicity. BMS-299897 is administered at 0.1-1 nmol/mouse, concomittantly with Aβ25-35 (9 nmol) in male Swiss mice. After one week, the contents in Aβ1-42 and Aβ1-40, and the levels in lipid peroxidation are analyzed in the mouse hippocampus. Mice are submitted to spontaneous alternation, passive avoidance and object recognition to analyze their short- and long-term memory abilities. Aβ25-35 increases Aβ1-42 content (+240%) but fails to affect Aβ1-40. BMS-299897 blocks the increase in Aβ1-42 content and decreased Aβ1-40 levels significantly. The compound does not affect Aβ25-35-induced increase in hippocampal lipid peroxidation. Behaviorally, BMS-299897 blocks the Aβ25-35-induced deficits in spontaneous alternation or novel object recognition, using a 1 h intertrial time interval. The co-administration of the γ-secretase inhibitor BMS-299897, in the 0.1-1 μmol/mouse dose-range, completely blocks the Aβ25-35-induced increase in Aβ1-42 content
参考文献: 1. Meunier J, et al. The γ-secretase inhibitor 2-[(1R)-1-[(4-chlorophenyl)sulfonyl](2,5-difluorophenyl) amino]ethyl-5-fluorobenzenebutanoic acid (BMS-299897) alleviates Aβ1-42 seeding and short-term memory deficits in the Aβ25-35 mouse model of Alzheimer's d 2. Weissmiller AM, et al. A γ-secretase inhibitor, but not a γ-secretase modulator, induced defects in BDNF axonal trafficking and signaling: evidence for a role for APP. PLoS One. 2015 Feb 24;10(2):e0118379.
溶解性: Soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.953 ml 9.767 ml 19.534 ml
5 mM 0.391 ml 1.953 ml 3.907 ml
10 mM 0.195 ml 0.977 ml 1.953 ml
50 mM 0.039 ml 0.195 ml 0.391 ml
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参考文献

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