Chemical Structure : ISM012-042
CAS No.:
2924181-80-4
ISM012-042
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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489.54
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Formula
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C25H27N7O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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tert-butyl 4-(6-(((6-cyanopyridin-3-yl)methyl)carbamoyl)-5-hydroxy-1,7-naphthyridin-2-yl)piperazine-1-carboxylate
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References
1. Fu Y, et al. Nat Biotechnol. 2024 Dec 11. doi: 10.1038/s41587-024-02503-w.
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