BU224 hydrochloride 是一种选择性高亲和力的咪唑啉imidazoline I2受体配体,Ki为 2.1 nM。BU224 hydrochloride 有时被用作 I2受体拮抗剂。BU224 hydrochloride 具有神经保护作用,具有抗炎、抗凋亡作用。BU224 hydrochloride 可改善 5XFAD 小鼠的记忆,增大树突棘和减少 Aβ 诱导的 NMDARs 的变化。BU224 hydrochloride 可用于阿尔茨海默病研究。
生物活性 | BU224 hydrochloride is a selective and high affinityimidazoline I2receptorligand, with aKiof 2.1 nM. BU224 hydrochloride is sometimes used as an I2receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research[1][2][3]. |
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体内研究 (In Vivo) | BU224 hydrochloride (5 mg/kg, IP, twice a day for 10 days) improves behavioural performance and memory function in 5XFAD mice[1]. BU224 hydrochloride (5 mg/kg, IP, twice a day for 10 days) reduces levels of the microglial marker Iba1 and pro-inflammatory cytokines IL-1β and TNF-α and increased the expression of astrocytic marker GFAP in 5XFAD mice[1]. BU224 hydrochloride (10 mg/kg, IP, once) reduces immobility of rats in the FST (forced swim test), indicative of antidepressant-like activity[2].
Animal Model: | 5XFAD mice and and WT littermates (6-month-old)[1] | Dosage: | 0 mg/kg, 5 mg/kg | Administration: | IP, twice a day for 10 days | Result: | Significantly increased immobility (54% increased freezing), and reversed memory deficits secondary to the deposition of Aβ in the brain. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : 12.5 mg/mL(53.49 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 4.2790 mL | 21.3950 mL | 42.7899 mL | 5 mM | 0.8558 mL | 4.2790 mL | 8.5580 mL | 10 mM | 0.4279 mL | 2.1395 mL | 4.2790 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 (protect from light)。-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: ≥ 1.25 mg/mL (5.35 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (5.35 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 12.5 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: ≥ 1.25 mg/mL (5.35 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (5.35 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 12.5 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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