规格 | 价格 | 库存 | 数量 |
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1mg |
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5mg |
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Other Sizes |
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体外研究 (In Vitro) |
spadin TFA(100 nM;COS-7 细胞)表现出 spadin 对 TREK-1 通道的抑制作用,它还能阻断花生四烯酸诱导的 63% 的 TREK-1 电流 [1]。在野生型小鼠脑切片中,spadin TFA (100 nM) 抑制 CA3 海马神经元中的 TREK-1 通道活性 [1]。
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体内研究 (In Vivo) |
在中缝背核 (DRN) 中,spadin TFA(10 μM,100 μL;腹腔注射;30 分钟;雄性 C57Bl/6J 和 TREK-1 缺陷小鼠)可增强 5-HT 神经元放电的速率 [2]。在小鼠中观察到 spadin TFA(0.01-100 μM,100 μL;脑室内、腹膜内和 ICV;每天一次,持续 7 天;雄性 C57Bl/6J 和 TREK-1 缺陷小鼠)的抗抑郁作用 [2]。
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动物实验 |
Animal/Disease Models: Male C57Bl/6J and TREK-1 deficient mice[2]
Doses: 10 μM Route of Administration: intraperitoneal (ip)injection; for 30 min Experimental Results: Increased of the 5-HT neuron firing rate in the dorsal raphe nucleus (DRN). Animal/Disease Models: Male C57Bl/6J and TREK-1 deficient mice[2] Doses: 0.01-100 μM Route of Administration: Intracerebroventrical injection (100 nM), intraperitoneal (ip)injection (1-100 μM) and intravenous (iv) injection (0.01-1 μM); daily, for 7 days Experimental Results: Had any effect on mouse locomotion analyzed in short- or long-time after the drug injection. |
参考文献 |
[1]. Borsotto M, et, al. Targeting two-pore domain K(+) channels TREK-1 and TASK-3 for the treatment of depression: a new therapeutic concept. Br J Pharmacol. 2015 Feb;172(3):771-84.
[2]. Mazella J, et, al. Spadin, a sortilin-derived peptide, targeting rodent TREK-1 channels: a new concept in the antidepressant drug design. PLoS Biol. 2010 Apr 13;8(4):e1000355. |
分子式 |
C92H143F3N26O24
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分子量 |
2126.36
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相关CAS号 |
Spadin;1270083-24-3
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溶解度 (体外) |
H2O :~25 mg/mL (~11.76 mM)
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (23.51 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
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 |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。