PRE-084 hydrochloride 是一种高选择性的σ1 受体 (S1R) 激动剂，其IC50值为 44 nM。PRE-084 hydrochloride 具有较好的神经保护作用，可改善小鼠的运动功能和运动神经元的存活率。PRE-084 hydrochloride 还能通过激活 Akt-eNOS 途径来改善大鼠心肌缺血再灌注损伤。
| 生物活性 | PRE-084 hydrochloride is a highly selectiveσ1 receptor(S1R) agonist, with anIC50of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway[1][2][3][4]. |
体外研究
(In Vitro) | PRE-084 hydrochloride (0.1-100 μM; 24 h) protects cultured cortical neurons against β-amyloid toxicity (maximally neuroprotective at 10 μM) and reduces the levels of proapoptotic protein Bax at 10 μM[1].
Cell Viability Assay[1] | Cell Line: | Cortical cells (βAP(25-35)-induced neurotoxicity model) | | Concentration: | 0.1-100 μM | | Incubation Time: | 24 h | | Result: | Reduced neuronal toxicity in a bell shaped-manner and is maximally neuroprotective at 10 μM. |
Western Blot Analysis[1] | Cell Line: | Cortical cells (βAP(25-35)-induced neurotoxicity model) | | Concentration: | 10 μM | | Incubation Time: | 24 h | | Result: | Reduced the levels of proapoptotic protein Bax in cortical neurons induced by βAP(25-35). |
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体内研究
(In Vivo) | PRE-084 hydrochloride (0.25 mg/kg; i.p.; 3 times a week for 8 weeks) displays beneficial effects on motor performance (improves motor neuron survival, ameliorates paw abnormality and grip strength performance) in wobbler mice, and shows neuroprotective effects (increases the levels of BDNF in the gray matter)[2].
PRE-084 hydrochloride (1 mg/kg; i.p.; single) protects the heart by activating the Akt-eNOS pathway in myocardial infarction model[3].
| Animal Model: | Wobbler mice (4-week-old)[2]. | | Dosage: | 0.25 mg/kg | | Administration: | Intraperitoneal injection; 3 times a week for 8 weeks. | | Result: | Significantly improved ameliorated paw abnormality from week 4, and notably improved paw grip strength at week 5.
Reduced the number of reactive astrocytes whereas increased the number of pan-macrophage marker CD68-positive cells and CD206+ cells involved in tissue restoration.
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| Animal Model: | Adult male Sprague-Dawley rats (220-250 g; myocardial infarction model)[3]. | | Dosage: | 1 mg/kg | | Administration: | Intraperitoneal injection; single. | | Result: | Significantly decreased the degree of myocardial apoptosis.
Led to significantly increased expression of p-Akt and p-eNOS. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 34 mg/mL(96.08 mM) H2O : 33.33 mg/mL(94.18 mM;ultrasonic and warming and heat to 60℃) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.8258 mL | 14.1291 mL | 28.2582 mL | | 5 mM | 0.5652 mL | 2.8258 mL | 5.6516 mL | | 10 mM | 0.2826 mL | 1.4129 mL | 2.8258 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 (sealed storage, away from moisture)。-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: ≥ 2.08 mg/mL (5.88 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.88 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.88 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.88 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.88 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.88 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。 *以上所有助溶剂都可在本网站选购。
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