ISM012-042

Chemical Structure : ISM012-042

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货号: PC-23633Not For Human Use, Lab Use Only.

ISM012-042 is a potent, orally gut-restricted, selective PHD1 and PHD2 inhibitor with IC50 of 1.9 nM and 2.5 nM for PHD1 hydroxylase and PHD2 hydroxylase, respectively.

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生物&药学活性

ISM012-042 is a potent, orally gut-restricted, selective PHD1 and PHD2 inhibitor with IC50 of 1.9 nM and 2.5 nM for PHD1 hydroxylase and PHD2 hydroxylase, respectively.
ISM012-042 exhibits gut-restricted pharmacokinetic (PK) properties, excellent activity and specificity against PHDs.
ISM012-042 resolves colitis, restores intestinal barrier function and reprograms the colonic immune environment.
ISM012-042 inhibited PHDs independently of extracellular iron levels and exerted anticolitis activity at markedly lower doses than SOC treatment mesalamine.
ISM012-042 attenuated colitis by restoring intestinal barrier function and alleviating intestinal inflammation.

物理化学性质&存储条件

分子量	489.54
分子式	C25H27N7O4
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	tert-butyl 4-(6-(((6-cyanopyridin-3-yl)methyl)carbamoyl)-5-hydroxy-1,7-naphthyridin-2-yl)piperazine-1-carboxylate

参考文献

1. Fu Y, et al. Nat Biotechnol. 2024 Dec 11. doi: 10.1038/s41587-024-02503-w.

ISM012-042

生物&药学活性

物理化学性质&存储条件

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ISM012-042

生物&药学活性

物理化学性质&存储条件

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