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)[1]. J-147 can inhibitmonoamine oxidaseB(MAO B) and thedopamine transporterwithEC50values of 1.88 μM and 0.649 μM, respectively[2]. J-147 has potential for the treatment of Alzheimer’s disease (AD)[3]. |
| IC50& Target | MAO B; Dopamine transporter[2] |
体外研究
(In Vitro) | J-147 promotes HT22 and primary cell survival in a dose-dependent manner (EC50value range of 0.06-0.115 μM)[2].
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体内研究
(In Vivo) | 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 (t1/2) 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)[2].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(285.44 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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