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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-Z218484536
Z218484536

Chemical Structure : Z218484536

CAS No.: 1223877-07-3

Z218484536

货号: PC-24886Not For Human Use, Lab Use Only.

Z218484536 is a potent and specific phosphoserine phosphatase (PSPH) inhibitor, inhibits the release of L-serine from cultured astrocytes with IC50 of 0.4 uM, reduces cellular L-serine levels with IC50 of 0.38 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Z218484536 is a potent and specific phosphoserine phosphatase (PSPH) inhibitor, inhibits the release of L-serine from cultured astrocytes with IC50 of 0.4 uM, reduces cellular L-serine levels with IC50 of 0.38 uM.
Z218484536 is highly selective against a panel of 20 protein tyrosine phosphatases, with only a weak inhibitory effect on DUSP22 at 30 uM.
Z218484536 has binding affinity for the A51V;G110A PSPH mutant (PSPH-MT) (6.1 uM), 26-fold lower than that for WT PSPH.
Z218484536 (2 mg/kg, i.p.) significantly reduced hippocampal levels of l-serine and d-serine in KA-induced chronic TLE mouse model.
Z218484536 (4 mg/kg) exhibited antiseizure effects in the KA mouse model of chronic temporal lobe epilepsy (TLE), also effectively reduced epileptic activity in the cynomolgus monkey TLE model.

物理化学性质&存储条件

分子量 247.23
分子式 C11H10FN5O
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

(E)-2-((3-(4-fluorophenyl)-1H-pyrazol-4-yl)methylene)hydrazine-1-carboxamide

参考文献

1. Sha L, et al. Nat Chem Biol. 2025 Jun 2. doi: 10.1038/s41589-025-01920-5.

2. Patent CN119367357 A 2025-01-28.

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