VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50 s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively.

2025年3月28日 · VP3.15 is a small heterocyclic drug-like molecule with safety profile and good pharmacodynamic and pharmacokinetic properties after intraperitoneal administration in different in vivo models [32].

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2022年11月19日 · In our study, VP3.15 ameliorates the disease course improving motor deficits of infected mice. Chronic treatment with VP3.15 also showed significant efficacy in the immunomodulation process, as well as in the proliferation and differentiation of oligodendroglial precursors, improving the preservation of myelin and axonal integrity.

VP3.15 is a small, heterocyclic molecule of the 5-imino-1,2,4-thiadiazole family with a dual action as a phosphodiesterase 7 and glycogen synthase kinase-3β (GSK-3β) inhibitor. VP3.15 reduces neuroinflammation and neuronal loss in other neurodegenerative disorders and might ameliorate complications associated with GM-IVH.

VP3.15 is a small, heterocyclic molecule of the 5-imino-1,2,4-thiadiazole family with a dual action as a phosphodiesterase 7 and glycogen synthase kinase-3β (GSK-3β) inhibitor. VP3.15 reduces neuroinflammation and neuronal loss in other neurodegenerative disorders and might ameliorate complications associated with GM-IVH.

Treatment of EAE mice with the novel PDE7i, VP3.15 showed more efficacy in reducing clinical signs at 10mgkg-1 than the other PDE7i, BRL50481 and similar to fingolimod. VP3.15 acts on peripheral lymphocytes inhibiting their proliferation and TNFα secretion in …

本研究使用一种小分子化合物VP3.15，它是一种5-亚氨基-1,2,4-噻二唑类的磷酸二酯酶7和糖原合成酶激酶3β（GSK-3β）抑制剂。 研究人员将VP3.15注入小鼠GM-IVH模型中，结果发现VP3.15可以减少短期（P14）和长期（P110）内出血和小胶质细胞的存在。 它可以改善脑萎缩和脑室扩大，同时限制tau过度磷酸化和神经元及髓鞘蛋白的损失。 VP3.15还可以提高神经元增殖和神经发生，以及缓解受损后的认知障碍。 有趣的是，VP3.15治疗后，血浆凝胶蛋白水平，即一种可行 …