Spadin TFA 是一种从血液中释放的前肽衍生的天然肽,是一种有效的 TREK-1 通道阻滞剂,其IC50值为 10 nM。Spadin TFA 增强小鼠中缝背核 5-HT 神经传递,诱导海马 CREB 激活和神经发生。Spadin TFA 可用于抗抑郁研究。
生物活性 | Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potentTREK-1 channelblocker with anIC50value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research[1][2]. |
体外研究 (In Vitro) | Spadin TFA (100 nM; COS-7 cells) has inhibitory effect of spadin on the TREK-1 channel and blocks 63% of the TREK-1 current stimulated by arachidonic acid[1]. Spadin TFA (100 nM) blocks the TREK-1 channels activity in CA3 hippocampal neurons on brain slices of wild-type mice[1].
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体内研究 (In Vivo) | Spadin TFA (10 μM, 100 μL; i.p.; for 30 min; male C57Bl/6J and TREK-1 deficient mice) increases of the 5-HT neuron firing rate in the dorsal raphe nucleus (DRN)[2]. Spadin TFA (0.01-100 μM, 100 μL; ICV, i.p. and i.v.; daily, for 7 days; male C57Bl/6J and TREK-1 deficient mice) has anti-depressant behavior in mice[2].
Animal Model: | Male C57Bl/6J and TREK-1 deficient mice[2] | Dosage: | 10 μM | Administration: | Intraperitoneal injection; for 30 min | Result: | Increased of the 5-HT neuron firing rate in the dorsal raphe nucleus (DRN). |
Animal Model: | Male C57Bl/6J and TREK-1 deficient mice[2] | Dosage: | 0.01-100 μM | Administration: | Intracerebroventrical injection (100 nM), intraperitoneal injection (1-100 μM) and intravenous injection (0.01-1 μM); daily, for 7 days | Result: | Had any effect on mouse locomotion analyzed in short- or long-time after the drug injection. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Sealed storage, away from moisture and light Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: H2O : 25 mg/mL(11.76 mM;Need ultrasonic) 配制储备液 1 mM | 0.4703 mL | 2.3514 mL | 4.7029 mL | 5 mM | 0.0941 mL | 0.4703 mL | 0.9406 mL | 10 mM | 0.0470 mL | 0.2351 mL | 0.4703 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 and 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: PBS Solubility: 50 mg/mL (23.51 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (1.18 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (1.18 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (1.18 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (1.18 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。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (1.18 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (1.18 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 25.0 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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