| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S86412-5mg买3赠1 |
99.00% | ￥310.00 |
>10 | - | - | - | - |
|
S86412-10mg买3赠1 |
99.00% | ￥408.00 |
9 | - | - | - | - |
|
S86412-50mg买3赠1 |
99.00% | ￥1800.00 |
>10 | - | - | - | - |
|
| 产品描述： | PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 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 | ||||||||||||||||||||
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| 靶点： | Sigma Receptor;Akt;NO Synthase;Sigmareceptor | ||||||||||||||||||||
| 体外研究： | 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. Cell Viability Assay 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 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). | ||||||||||||||||||||
| 体内研究： | 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). PRE-084 hydrochloride (1 mg/kg; i.p.; single) protects the heart by activating the Akt‑eNOS pathway in myocardial infarction model. Animal Model: Wobbler mice (4-week-old). 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. 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. | ||||||||||||||||||||
| 参考文献： | 1. Marrazzo A, et al. Neuroprotective effects of sigma-1 receptor agonists against beta-amyloid-induced toxicity. Neuroreport. 2005 Aug 1;16(11):1223-6. 2. Peviani M, et al. Neuroprotective effects of the Sigma-1 receptor (S1R) agonist PRE-084, in a mouse model of motor neuron disease not linked to SOD1 mutation. Neurobiol Dis. 2014 Feb;62:218-32. 3. Gao QJ, et al. Sigma-1 Receptor Stimulation with PRE-084 Ameliorates Myocardial Ischemia-Reperfusion Injury in Rats. Chin Med J (Engl). 2018 Mar 5;131(5):539-543. 4. Su TP, et al. Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand. J Pharmacol Exp Ther. 1991 Nov;259(2):543-50. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO、H2O | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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