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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-VP3.15 dihydrobromide
VP3.15 dihydrobromide

Chemical Structure : VP3.15 dihydrobromide

CAS No.: 1281681-33-1

VP3.15 dihydrobromide

货号: PC-23484Not For Human Use, Lab Use Only.

VP3.15 dihydrobromide is a potent, oral bioavailable and CNS penetrant dual PDE7/GSK-3 inhibitor with IC50 of 1.59 uM (PDE7) and 0.88 uM (GSK-3).

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10 mg ¥1480 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

VP3.15 dihydrobromide is a potent, oral bioavailable and CNS penetrant dual PDE7/GSK-3 inhibitor with IC50 of 1.59 uM (PDE7) and 0.88 uM (GSK-3).
VP3.15 increases intracellular cAMP levels in cells.
VP3.15 is efficacious in the amelioration of the clinical symptoms in EAE mice.
VP3.15 improves in vivo remyelination in mouse and increases both adult mouse and adult human oligodendrocyte progenitor cell (OPC) differentiation, in addition to its immune regulatory action.
VP3.15's dual inhibition is synergistic, as increasing intracellular levels of cAMP by cyclic nucleotide PDE inhibition both suppresses the immune response and increases remyelination, and in addition, inhibition of GSK3 limits experimental autoimmune encephalomyelitis in mice.

物理化学性质&存储条件

分子量 528.31
分子式 C20H24Br2N4OS
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-Morpholinoethyl)-2,3-diphenyl-1,2,4-thiadiazol-5(2H)-imine dihydrobromide

参考文献

1. Martín-Álvarez R, et al. J Chem Neuroanat. 2017 Mar;80:27-36.

2. Medina-Rodríguez EM, et al. Sci Rep. 2017 Mar 3;7:43545.

3. Sánchez-Cruz A, et al. Mol Neurodegener. 2018 Apr 16;13(1):19.

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