PROFILPELAJAR.COM

ML148

ML148
Clinical data
Drug class15-PGDH inhibitor
Identifiers
  • [1-(3-methylphenyl)benzimidazol-5-yl]-piperidin-1-ylmethanone
CAS Number
PubChem CID
ChemSpider
ChEBI
ChEMBL
Chemical and physical data
FormulaC20H21N3O
Molar mass319.408 g·mol−1
3D model (JSmol)
  • CC1=CC(=CC=C1)N2C=NC3=C2C=CC(=C3)C(=O)N4CCCCC4
  • InChI=1S/C20H21N3O/c1-15-6-5-7-17(12-15)23-14-21-18-13-16(8-9-19(18)23)20(24)22-10-3-2-4-11-22/h5-9,12-14H,2-4,10-11H2,1H3
  • Key:YQNOQZALLOQMPY-UHFFFAOYSA-N

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

  1. ^ 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.
  2. ^ 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.
  3. ^ 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.

Content Disclaimer

Informasi ini disarikan dari Wikipedia dan disajikan kembali untuk tujuan edukasi. Konten tersedia di bawah lisensi CC BY-SA 3.0. Kami tidak bertanggung jawab atas ketidakakuratan data yang bersumber dari kontribusi publik tersebut.

  1. The information displayed on this website is sourced in part or in whole from Wikipedia and has been adapted for the purpose of restating it. We strive to provide accurate and relevant information, however:
  2. There is no guarantee of absolute accuracy. Wikipedia is an open, collaborative project that can be edited by anyone, so information is subject to change.
  3. It is not intended to constitute professional advice. The content displayed is for informational and educational purposes only. For important decisions (e.g., medical, legal, or financial), please consult a professional.
  4. Content copyright. Wikipedia is licensed under the Creative Commons Attribution-ShareAlike License (CC BY-SA). This means that content may be reused with appropriate attribution and shared under a similar license.
  5. Responsible use. Any risk arising from the use of information from this website is entirely the responsibility of the user.