010-60605840
结构式搜索
  1. 首页
  2. 产品目录
  3. Signaling Pathways(信号通路)
  4. Neuronal Signaling(神经信号通路)
  5. γ-secretase
中文名称: BMS 299897
英文名称: BMS 299897
CAS No: 290315-45-6
分子式: C24H21ClF3NO4S
分子量: 511.94
安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)
B70157 BMS 299897 ≥98% (psaitong)
包装规格：
5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：
溶于DMSO(≥30mg/mL）
产品描述：

基本信息

产品编号：

B70157

产品名称：

BMS 299897

CAS:

290315-45-6

 

储存条件

粉末

-20℃

四年

 

 

分子式：

C24H21ClF3NO4S

溶于液体

-80℃

6个月

分子量

511.94

-20℃

1个月

化学名： 

2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl]-5-fluoro-benzenebutanoic acid

Solubility (25°C)：

 

体外:

 

DMSO

≥ 30 mg/mL (58.60mM)

Ethanol

 

Water

 

体内(现配现用):

1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline

Solubility: ≥ 2.5 mg/mL (4.88mM); Clear solution

此⽅案可获得 ≥ 2.5 mg/mL (4.88mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加⼊ 50μL Tween-80，混合均匀；然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。

＜1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

1.9534mL

9.7668mL

19.5335mL

5mM

0.3907mL

1.9534mL

3.9067mL

10mM

0.1953mL

0.9767mL

1.9534mL

 

生物活性

产品描述

一种磺胺类γ-secretase 抑制剂，作用于稳定过表达淀粉样前体蛋白 (APP) 的HEK293 细胞，抑制Aβ产生，IC50 为 7nM。

靶点

IC50: 7nM (Aβ, in HEK293 cells)

体外研究

BMS-299897 reduces the levels of each of the Aβ peptides. At 1μM, BMS-299897 decreases these peptides to levels ranging from 20 to 50% of the vehicle control. BMS-299897 treatment reduces the portion of QD-BDNF signals moving in the retrograde direction (p=0.0198) with a concomitant increase in the portion of signals moving in the anterograde direction (p=0.0147).

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 γsecretase 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 Aβ 1-40, 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 doserange, completely blocks the Aβ25-35-induced increase in Aβ1-42 content.

 

推荐实验方法(仅供参考)

Cell Assay

Neuronal cultures are treated at indicated DIVs for 24 hrs with 1μM BMS-299897, 2.5μM sGSM41 or the vehicle DMSO (final concentration: 0.1%) for most of the experiments, or for different periods of time as indicated in specific experiments. Transfections of siRNAs are performed on 100,000 neurons at DIV4 using NTER Nanoparticle transfection system following the protocol provided. The siRNAs used are: 1) siRNA against rat APP, and 2) the MISSION siRNA. Knockdown experiments are optimized by examining both mRNA and protein expression of APP. A knockdown efficiency of 80% at the mRNA level as quantitated with the 7300 Real Time PCR System and 30% at the protein level by immunoblotting is routinely achieved.

 

Animal Administration

Mice

 Male Swiss OF 1 mice, aged 7-9 weeks and weighing 32±2 g are used. Doses of 0.1, 0.3 and 1μmol are injected i.c.v. in 1μL simultaneously with the Aβ25-35 peptide. Animals are used at day 7-9 after i.c.v. injections for behavioral testing or sacrifice, before biochemical measures. All experiments are conducted on separate batch of mice, except spontaneous alternation and passive avoidance, which are done in series in the same animals
保存条件：
-20℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
购物指南
参考资料
支付方式
关于配送
售后服务
微信二维码
首页 |网站使用条款 |隐私政策 |关于我们 |营业执照 |结构式搜索
© 2001-2020 北京普西唐生物科技有限公司  天津普西唐生物医药科技有限公司
版权所有，并保留所有权利 
备案号：京ICP备17064988号-1