hCES2A inhibitor 14n

Chemical Structure : hCES2A inhibitor 14n

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货号: PC-24238Not For Human Use, Lab Use Only.

hCES2A inhibitor 14n is a potent, selective and covalent human carboxylesterase 2A (hCES2A) inhibitor with IC50 of 0.04 nM.

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生物&药学活性

hCES2A inhibitor 14n is a potent, selective and covalent human carboxylesterase 2A (hCES2A) inhibitor with IC50 of 0.04 nM.
hCES2A inhibitor 14n actsas a covalent inhibitor of hCES2A by specifically targeting the catalytic serine residue Ser-228.
hCES2A inhibitor 14n demonstrates relatively weak inhibition of hCES1A (IC50 = 4403 nM) and hBuChE (IC50 = 3063 nM), while exhibiting negligible inhibition of hNotum, hPL, hThrombin, and hDPP-IV at 10 uM.
hCES2A inhibitor 14n possesses good cell membrane penetrability and remarkable inhibitory effects on intracellular hCES2A。
hCES2A inhibitor 14n significantly ameliorate irinotecan-triggered gut toxicity (ITGT) without diminishing the anti-tumor effects of irinotecan in tumor-bearing mice.

物理化学性质&存储条件

分子量	410.51
分子式	C24H30N2O4
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	4-(4-Benzylpiperidine-1-carbonyl)-2-methoxyphenyl ethyl(methyl)carbamate

参考文献

1. Sang Z, et al. J Med Chem. 2025 Mar 12. doi: 10.1021/acs.jmedchem.4c02560.