2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase
  4. Begacestat

Begacestat  (Synonyms: GSI-953)

目录号: HY-14175 纯度: 99.29%
COA 产品使用指南

摩尔计算器

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。

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Begacestat Chemical Structure

Begacestat Chemical Structure

CAS No. : 769169-27-9

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1100
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1 mg ￥800
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5 mg ￥1280
In-stock
10 mg ￥2050
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25 mg ￥4100
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Customer Review

Begacestat 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target

IC50: 15 nM (Aβ40)[1].
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
14.8 nM
Compound: 16; GSI-953
Inhibition of gamma secretase (unknown origin) mediated APP cleavage in CHO cells expressing APP Swedish KM/NL mutant assessed as reduction in amyloid beta 40 after 24 hrs by sandwich ELISA
Inhibition of gamma secretase (unknown origin) mediated APP cleavage in CHO cells expressing APP Swedish KM/NL mutant assessed as reduction in amyloid beta 40 after 24 hrs by sandwich ELISA
[PMID: 27045975]
CHO ED50
350 nM
Compound: 42
Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay
Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay
[PMID: 23713656]
CHO IC50
353 nM
Compound: GSI-953
Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay
Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay
[PMID: 23312944]
CHO ED50
7.8 nM
Compound: 42
Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA
Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA
[PMID: 23713656]
HEK293 ED50
7.8 nM
Compound: GSI-953
Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis
Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis
[PMID: 23312944]
IMR-32 IC50
1.6 nM
Compound: GSI-953
Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA
Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA
[PMID: 23312944]
IMR-32 IC50
10.5 nM
Compound: GSI-953
Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA
Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA
[PMID: 23312944]
SH-SY5Y IC50
8 nM
Compound: 62, Begacestat
Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay
Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay
[PMID: 19694467]
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
分子量

391.74

Formula

C9H8ClF6NO3S2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (127.64 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5527 mL 12.7636 mL 25.5271 mL
5 mM 0.5105 mL 2.5527 mL 5.1054 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.38 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.38 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.29%

COA (288 KB) LCMS (84 KB)

产品使用指南 (1538 KB)
参考文献

Begacestat 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5527 mL 12.7636 mL 25.5271 mL 63.8178 mL
5 mM 0.5105 mL 2.5527 mL 5.1054 mL 12.7636 mL
10 mM 0.2553 mL 1.2764 mL 2.5527 mL 6.3818 mL
15 mM 0.1702 mL 0.8509 mL 1.7018 mL 4.2545 mL
20 mM 0.1276 mL 0.6382 mL 1.2764 mL 3.1909 mL
25 mM 0.1021 mL 0.5105 mL 1.0211 mL 2.5527 mL
30 mM 0.0851 mL 0.4255 mL 0.8509 mL 2.1273 mL
40 mM 0.0638 mL 0.3191 mL 0.6382 mL 1.5954 mL
50 mM 0.0511 mL 0.2553 mL 0.5105 mL 1.2764 mL
60 mM 0.0425 mL 0.2127 mL 0.4255 mL 1.0636 mL
80 mM 0.0319 mL 0.1595 mL 0.3191 mL 0.7977 mL
100 mM 0.0255 mL 0.1276 mL 0.2553 mL 0.6382 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Begacestat769169-27-9GSI-953GSI953GSI 953γ-secretaseGamma secretaseInhibitorinhibitorinhibit

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