BrBzGCp2 是乙二醛酶 1(GLO1)的抑制剂，其GC50为 4.23 μM (HL-60 细胞)。BrBzGCp2 具有抗肿瘤和神经保护活性。
| 生物活性 | BrBzGCp2 is aGlyoxalase1 (GLO1)inhibitor, with aGC50of 4.23 μM in HL-60 cells. BrBzGCp2 possesses antitumor and neuroprotective activity[1][2].
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体内研究
(In Vivo) | GLO1 inhibition by BrBzGCp2 increases center time in the OF test, without changing distance traveled. GLO1 inhibition increases MG (methylglyoxal) concentration, thus reducing anxiety-like behavior[2].
BrBzGCp2 pre-treatment decreases seizure duration[3].
BrBzGCp2 injection alleviates the level of anxiety in mice, and mice with less anxiety and fear were more likely to explore the unknown area, implying that inhibition of GLO1 activity mitigated anxiety levels[4].
BrBzGCp2 treatment restores the VPA-induced inhibition effect on GABAAreceptor activation[4].
BrBzGCp2 significantly lowers the blood pressure and ameliorated endothelial dysfunction in diabetic mice[5].
| Animal Model: | Male CD-1 mice[2]. | | Dosage: | 50 mg/kg. | | Administration: | IP once (Two hours post-injection, mice were sacrificed, and brains were rapidly dissected and flash-frozen on dry ice. MG concentration was measured) | | Result: | Allowed MG levels to accumulate for 2 hours |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(408.11 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.6324 mL | 8.1622 mL | 16.3244 mL | | 5 mM | 0.3265 mL | 1.6324 mL | 3.2649 mL | | 10 mM | 0.1632 mL | 0.8162 mL | 1.6324 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 (stored under nitrogen)。-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： 8% DMSO 18%Tween-80 74% saline Solubility: 20 mg/mL (32.65 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (3.40 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.40 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 (3.40 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.40 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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