Begacestat GSI-953|cas:769169-27-9|西域试剂

Begacestat GSI-953,99.56%

产品编号：Bellancom-14175| CAS NO：769169-27-9| 分子式：C₉H₈ClF₆NO₃S₂| 分子量：391.74

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货号	价格	库存与货期
Bellancom-14175	￥800.00	杭州北京（现货）
Bellancom-14175	￥1280.00	杭州北京（现货）
Bellancom-14175	￥2050.00	杭州北京（现货）
Bellancom-14175	￥4100.00	杭州北京（现货）
Bellancom-14175	￥6560.00	杭州北京（现货）

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Begacestat GSI-953

产品介绍

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。

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.

体外研究

体内研究

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).
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.

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

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.

体内研究

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

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (127.64 mM; Need ultrasonic)

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
10 mM	0.2553 mL	1.2764 mL	2.5527 mL

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。

In Vivo:

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

1.

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); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.38 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

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); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.38 mM，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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.38 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。