ANA-12是有效，选择性的 TrkB 拮抗剂，对高亲和力和低亲和力位点的IC₅₀ 分别为45.6 nM和41.1 μM。

ANA-12 is a potent and selective TrkB antagonist with IC 50 s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively.

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ANA-12 (10 nM) prevents BDNF-induced neurite outgrowth in the TrkB-expressing cells, and completely abolishes the effects of BDNF at concentrations up to 10-100 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

ANA-12 (0.5 mg/kg, i.p.) partially inhibits the total endogenous TrkB activity in the whole brain of mice. ANA-12, injected in mice, demonstrates anxiolytic and antidepressive activities at 0.5 mg/kg. ANA-12 (0.5, 1.0, and 2.0 mg/kg) does not affect neuron survival. ANA-12 (0.5 mg/kg) shows antidepressant effects in lipopolysaccharide (LPS)-induced depression-like behavior. ANA-12 (0.5 mg/kg) significantly attenuates an increased immobility time in depressed mice. In the TST, FST, and SPT, ANA-12 (0.5 mg/kg) does not show antidepressant-like effects in the control mice. ANA-12 (0.5 mg/kg, i.p.) reverses the diminished self-administration of cocaine in CocSired rats. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Cazorla M, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest. 2011 May;121(5):1846-57.
[2]. Fang X, et al. Brain-derived neurotrophic factor-TrkB signaling in the medial prefrontal cortex plays a role in the anhedonia-like phenotype after spared nerve injury. Eur Arch Psychiatry Clin Neurosci. 2018 Jun 7.

In Vitro: DMSO : 9.09 mg/mL (22.31 mM; Need ultrasonic)Ethanol : < 1 mg/mL (ultrasonic) (insoluble)配制储备液