Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC 50 value 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.
性状
Solid
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.Spadin TFA (100 nM) blocks the TREK-1 channels activity in CA3 hippocampal neurons on brain slices of wild-type mice. has not independently confirmed the accuracy of these methods. They are for reference only.
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).
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and lightPowder -80°C 2 years;-20°C 1 year
SequenceShortening
YAPLPRWSGPIGVSWGLR
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.
溶解度数据
In Vitro: H2O : 25 mg/mL (11.76 mM; Need ultrasonic)配制储备液