化合物 Hcyb1 T61617

Product Introduction
Bioactivity


英文名: Hcyb1

描述: Hcyb1 is a potent and specific inhibitor of phosphodiesterase 2 (PDE2). It exhibits a high degree of selectivity for inhibiting PDE2A with an IC50 value of 0.57 μM. In addition, Hcyb1 displays over 250-fold selectivity against other recombinant members of the PDE family. Moreover, its pharmacological actions include neuroprotective and antidepressant-like effects, which are believed to be mediated through the cAMP/cGMP-CREB-BDNF signaling pathway [1].

体外活性: Hcyb1 increases cGMP levels by 1.7~2.3 folds after 10-minute treatment at concentrations of 1~100 nM [1]. Hcyb1 increases both cGMP and cAMP levels 24 hours after treatment at the concentrations of 1 nM [1]. Hcyb1 treatment also increases the levels of phosphorylation of CREB and BDNF in HT-22 cells for 24 hours [1]. Hcyb1 promotes HT-22 cell viability and increase the cGMP and cAMP accumulation in HT-22 cells [1]. Hcyb1 exhibits the concentration- and time-dependent effects on cell viability in HT-22 cells [2]. Cell Proliferation Assay [1] Cell Line: HT-22 cells Concentration: 1 pM, 0.01 nM, 0.1 nM, 1 nM, 0.01 μM, 0.1 μM, 1 μM, 10 μM Incubation Time: 24 hours Result: The cell viability was significantly increased when treatment HT-22 cells with Hcyb1 at concentrations of 0.1 nM and 1 nM for 24 hours. The time-dependent effects showed that the cell viability was significantly increased from 12 to 24 hours when treatment at concentration of 1 nM. The maximal effects peaked at 24 hours after treatment. Western Blot Analysis [1] Cell Line: HT-22 cells Concentration: 1 nM Incubation Time: 24 hours Result: Induced a significant increase in the phosphorylation of CREB. BDNF expression was also significantly upregulated at the same concentration.

体内活性: Hcyb1 (0.5, 1, and 2 mg/kg, i.g.) decreases the immobility time in both forced swimming and tail suspension tests, without altering locomotor activity [3]. Animal Model: Male imprinting control region (ICR) mice, weighing between 20 and 25 g [3] Dosage: 0.5, 1, and 2 mg/kg Administration: Gavage (i.g.) Result: Exhibited dose-dependent reduction in immobility time at doses of 0.5, 1, 2 mg/kg (i.g.).

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途