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HTL26119

HTL26119
Clinical data
ATC code
  • None
Identifiers
  • 5-[4-[2,4-dichloro-6-[4-[2-(4-chloropyrazol-1-yl)ethoxy]phenyl]phenoxy]phenyl]-4-oxopentanoic acid
PubChem CID
Chemical and physical data
FormulaC28H23Cl3N2O5
Molar mass573.85 g·mol−1
3D model (JSmol)
  • C1=CC(=CC=C1CC(=O)CCC(=O)O)OC2=C(C=C(C=C2Cl)Cl)C3=CC=C(C=C3)OCCN4C=C(C=N4)Cl
  • InChI=1S/C28H23Cl3N2O5/c29-20-14-25(19-3-8-23(9-4-19)37-12-11-33-17-21(30)16-32-33)28(26(31)15-20)38-24-6-1-18(2-7-24)13-22(34)5-10-27(35)36/h1-4,6-9,14-17H,5,10-13H2,(H,35,36)
  • Key:DGUBCYZSWLRFKT-UHFFFAOYSA-N

HTL26119 is a drug which acts as a potent and selective negative allosteric modulator behaving as a functional antagonist of the glucagon-like peptide-1 receptor (GLP-1). While GLP-1 receptor agonists are widely used for the treatment of obesity and diabetes, there are few antagonists known for this receptor. However, these also have potential medical uses for indications where weight gain is desirable, such as treatment of sarcopenia in the elderly and cachexia in patients affected by conditions such as cancer and AIDS. While HTL26119 itself is unlikely to be developed for medical use, as one of the first selective antagonists for GLP-1 it has been widely used as a pharmacological tool compound for the study of the GLP-1 receptor and its signaling pathway.[1][2][3]

See also

References

  1. ^ O'Brien A, Andrews SP, Baig AH, Bortolato A, Brown AJ, Brown GA, et al. (15 October 2019). "Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure- based drug design". Bioorganic & Medicinal Chemistry Letters. 29 (20) 126611. doi:10.1016/j.bmcl.2019.08.015. PMID 31447084.
  2. ^ Zhou Q, Guo W, Dai A, Cai X, Vass M, de Graaf C, et al. (23 June 2021). "Discovery of novel allosteric modulators targeting an extra-helical binding site of GLP-1R using structure-and ligand-based virtual screening". Biomolecules. 11 (7): 929. doi:10.3390/biom11070929. PMC 8301998.
  3. ^ Bortolato A, Mason JS (2022-03-07). "Discovery of HTL26119". Contemporary Accounts in Drug Discovery and Development: 179–200. doi:10.1002/9781119627784.ch9. ISBN 978-1-119-62778-4.{{cite journal}}: CS1 maint: periodical has ISBN (link)
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