// Workers AI · dad joke modeWhat did HTL26119 say to its date? "You're a byte above the rest.

HTL26119
Clinical data
ATC code	None;
Identifiers
	IUPAC name 5-[4-[2,4-dichloro-6-[4-[2-(4-chloropyrazol-1-yl)ethoxy]phenyl]phenoxy]phenyl]-4-oxopentanoic acid;
PubChem CID	172873530;
Chemical and physical data
Formula	C28H23Cl3N2O5
Molar mass	573.85 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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]

References

↑ 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.
↑ 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.
↑ 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.

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[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.

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// Workers AI · dad joke modeWhat did HTL26119 say to its date? "You're a byte above the rest.

See also

References