ELN318463|cas:851600-86-7|西域试剂

ELN318463,99.45%

产品编号：Bellancom-50882| CAS NO：851600-86-7| 分子式：C₁₉H₂₀BrClN₂O₃S| 分子量：471.80

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货号	价格	库存与货期
Bellancom-50882	￥8000.00	杭州北京（现货）
Bellancom-50882	￥13000.00	杭州北京（现货）
Bellancom-50882	￥35000.00	杭州北京（现货）
Bellancom-50882	￥49000.00	杭州北京（现货）

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ELN318463

产品介绍

ELN318463 是淀粉样前体蛋白 (APP) 选择性的 γ-分泌酶 (γ-secretase) 抑制剂。ELN318463 对包含早老蛋白 (PS1) 和 PS2 的 γ-分泌酶抑制活性不同，对 PS1 和 PS2 的 EC₅₀ 分别为 12 nM 和 656 nM。ELN318463 对 PS1 的选择性比对 PS2 高约 51 倍。

生物活性

ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC₅₀s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 is 51-fold more selective for PS1.

体外研究

ELN318463 behaves as a classic γ-secretase inhibitor, demonstrates 75- to 120-fold selectivity for inhibiting Aβ production compared with Notch signaling in cells, and displaces an active site directed inhibitor at very high concentrations only in the presence of substrate.

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

体内研究

ELN318463 (30 mg/kg or 100 mg/kg; orally) leads acute reduction of brain Aβ in in the PDAPP transgene model of Alzheimer's disease (AD) as well as in wild-type FVB strain mice.

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

Animal Model:	Female, two- to three-month old, FVB/N mice and PDAPP transgene model of Alzheimer's disease (AD)
Dosage:	30 mg/kg or 100 mg/kg
Administration:	Orally
Result:	Brain levels at 30 mg/kg were 0.754 μM in FVB brains and 0.69 μM in PDAPP brains, and at 100 mg/kg dose the levels were 2.7 μM in FVB brains and 1.87 μM in PDAPP brains.

体内研究

ELN318463 (30 mg/kg or 100 mg/kg; orally) leads acute reduction of brain Aβ in in the PDAPP transgene model of Alzheimer's disease (AD) as well as in wild-type FVB strain mice.

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

Animal Model:	Female, two- to three-month old, FVB/N mice and PDAPP transgene model of Alzheimer's disease (AD)
Dosage:	30 mg/kg or 100 mg/kg
Administration:	Orally
Result:	Brain levels at 30 mg/kg were 0.754 μM in FVB brains and 0.69 μM in PDAPP brains, and at 100 mg/kg dose the levels were 2.7 μM in FVB brains and 1.87 μM in PDAPP brains.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (264.94 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1195 mL	10.5977 mL	21.1954 mL
5 mM	0.4239 mL	2.1195 mL	4.2391 mL
10 mM	0.2120 mL	1.0598 mL	2.1195 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: ≥ 2.08 mg/mL (4.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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% corn oil
Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.41 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。