LDN-212320 (LDN-0212320) 是谷氨酸转运体(GLT-1)/兴奋性氨基酸转运体 2(EAAT2)的激活剂。LDN-212320 (LDN-0212320) 通过上调海马和 ACC 星形胶质细胞 GLT-1 的水平来预防伤害性疼痛。
生物活性 | LDN-212320 (LDN-0212320) is aglutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2)activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC[1][2]. |
体内研究 (In Vivo) | LDN-212320 (10 or 20 mg/kg, i.p) significantly attenuates formalin-evoked nociceptive behavior[1]. LDN-212320 (10 or 20 mg/kg, i.p) significantly reverses formalin-induced impaired hippocampal-dependent behavior. In addition, LDN-212320 (10 or 20 mg/kg, i.p) increases GLT-1 expressions in the hippocampus and ACC[1]. LDN-212320 (20 mg/kg, i.p) significantly reduced formalin induced-ERK phosphorylation, a marker of nociception, in the hippocampus and ACC[1].
Animal Model: | Mice[1]. | Dosage: | 10 or 20 mg/kg. | Administration: | IP 24 h before the injection of formalin. | Result: | Significantly attenuated licking and biting behavior during both phases 1 and 2 in a dose-dependent manner compared to formalin-injected mice. Significantly (P< 0.01 or P< 0.001) reduced the licking and biting behavior. Significantly increased preference for the displaced object (F3, 13= 28.03, P< 0.01) compared to formalin-injected mice. Significantly (P< 0.001) increased interaction time with the displaced object compared to formalin-injected mice.
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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 : 50 mg/mL(170.42 mM;Need ultrasonic) 配制储备液 1 mM | 3.4084 mL | 17.0422 mL | 34.0843 mL | 5 mM | 0.6817 mL | 3.4084 mL | 6.8169 mL | 10 mM | 0.3408 mL | 1.7042 mL | 3.4084 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: ≥ 2.5 mg/mL (8.52 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.52 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (8.52 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.52 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 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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