J-147|cas:1146963-51-0|西域试剂

J-147,99.87%

产品编号：Bellancom-13779| CAS NO：1146963-51-0| 分子式：C₁₈H₁₇F₃N₂O₂| 分子量：350.34

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货号	价格	库存与货期
Bellancom-13779	￥1050.00	杭州北京（现货）
Bellancom-13779	￥1620.00	杭州北京（现货）
Bellancom-13779	￥4800.00	杭州北京（现货）

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J-147

产品介绍

J-147 是一种特别有效的，具有口服活性的神经保护剂，可增强认知能力。J-147 可透过血脑屏障 (BBB)。J-147 抑制单胺氧化酶 B (MAO B) 和多巴胺转运体 (dopamine transporter)，EC₅₀ 分别为 1.88 μM 和 0.649 μM。J-147 有潜力用于阿尔茨海默氏症 (AD) 的研究。

生物活性

J-147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J-147 can readily pass the blood brain barrier (BBB). J-147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC₅₀ values of 1.88 μM and 0.649 μM, respectively. J-147 has potential for the treatment of Alzheimer’s disease (AD).

体外研究

J-147 promotes HT22 and primary cell survival in a dose-dependent manner (EC₅₀ value range of 0.06-0.115 μM) .

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

体内研究

J-147 (diet is prepared by the addition of J-147 at 200ppm; 6 months) enhances memory and dendritic spine number in old mice^[4].
The half life (t_1/2) of J-147 is calculated at 1.5 hrs in plasma and 2.5 hrs in brain ( per oral (PO) administration at a single dose of 20 mg/kg).

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

Animal Model:	24 male C57Bl/6 mice aged 24 months; using 8 month-old mice as controls^[4]
Dosage:	200 ppm
Administration:	The diet was prepared by the addition of 200ppm; 6 months
Result:	While both young and old animals recognized when an object was moved a large distance (135 degrees), a reduction in the recognition index (RI) in aged mice was observed when the object was moved a smaller distance of 45 degrees. The reduction in the RI was reversed upon treatment with J147.

体内研究

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

Animal Model:	24 male C57Bl/6 mice aged 24 months; using 8 month-old mice as controls^[4]
Dosage:	200 ppm
Administration:	The diet was prepared by the addition of 200ppm; 6 months
Result:	While both young and old animals recognized when an object was moved a large distance (135 degrees), a reduction in the recognition index (RI) in aged mice was observed when the object was moved a smaller distance of 45 degrees. The reduction in the RI was reversed upon treatment with J147.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (285.44 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8544 mL	14.2718 mL	28.5437 mL
5 mM	0.5709 mL	2.8544 mL	5.7087 mL
10 mM	0.2854 mL	1.4272 mL	2.8544 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: ≥ 1.88 mg/mL (5.37 mM); Clear solution

此方案可获得 ≥ 1.88 mg/mL (5.37 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 18.8 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% (20% SBE-β-CD in saline)
Solubility: 1.88 mg/mL (5.37 mM); Suspended solution; Need ultrasonic

此方案可获得 1.88 mg/mL (5.37 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 18.8 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