ML148
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Pharmaceutical compound
| Clinical data | |
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| Drug class | 15-PGDH inhibitor |
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| Formula | C20H21N3O |
| Molar mass | 319.408g·mol−1 |
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ML148 is a drug which acts as a reasonably potent and selective inhibitor of the enzyme 15-hydroxyprostaglandin dehydrogenase (15-PGDH), with an IC50 of 56 nM. It increases levels of prostaglandin E2 and stimulates tissue regeneration. It was one of the earliest selective 15-PGDH inhibitors developed, and is now mainly significant as a lead compound which was used to develop more potent derivatives such as HW201877, but is still used in research as its simple chemical structure and straightforward synthesis makes it a cost-effective alternative to more complex compounds.[1] [2] [3]
References
- ↑ Jadhav A, Niesen FH, Schultz L, Oppermann U, Maloney DJ, Simeonov A (2010). "Potent and selective inhibitors of NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD)". Probe Reports from the NIH Molecular Libraries Program. Bethesda: National Center for Biotechnology Information. PMID 21735612.
- ↑ Niesen FH, Schultz L, Jadhav A, Bhatia C, Guo K, Maloney DJ, et al. (November 2010). "High-affinity inhibitors of human NAD-dependent 15-hydroxyprostaglandin dehydrogenase: mechanisms of inhibition and structure-activity relationships". PLOS ONE. 5 (11) e13719. Bibcode:2010PLoSO...513719N. doi:10.1371/journal.pone.0013719 . PMC 2970562 . PMID 21072165.
- ↑ Duveau DY, Yasgar A, Hu X, Kouznetsova J, Brimacombe KR, Kerns EH, et al. (2010). "Discovery of two small molecule inhibitors, ML387 and ML388, of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase". Probe Reports from the NIH Molecular Libraries Program. Bethesda: National Center for Biotechnology Information. PMID 25834895.
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