UPG-111

UPG-111 is a peptide compound that acts as a negative allosteric modulator of the Urotensin II receptor (UTR) . UPG-111 exhibits a dual inhibitory effect on the vasoconstriction induced by UTR agonists - it reduces both the maximum response intensity and the sensitivity of the agonist. UPG-111 does not induce calcium release or cause contraction of the endothelium-deprived rat aortic rings. UPG-111 can be used for the study of various diseases related to the angiotensinergic system[1].

Product Specifications

CAS Number

[3090687-02-5]

UNSPSC

12352209

Target

Urotensin Receptor

Related Pathways

GPCR/G Protein

Field of Research

Cancer; Metabolic Disease; Inflammation/Immunology; Cardiovascular Disease

Smiles

O=C([C@@H](NC([C@H](C(C)(SSC[C@H](NC([C@@H](NC([C@@H](NC1=O)CCCN)=O)CC2=CC=C(C=C2)O)=O)C(N[C@H](C(O)=O)C(C)C)=O)C)NC([C@H](CC(O)=O)NC([C@H]3N(CCC3)C([C@H]([C@H](O)C)NC([C@@H](N)CCO)=O)=O)=O)=O)=O)CC4=CC=CC=C4)N[C@@H]1CC5=CNC6=CC=CC=C56

Molecular Formula

C64H87N13O17S2

Molecular Weight

1374.58

References & Citations

[1]Merlino F, et al. Expanding Structure-Activity Relationships of Human Urotensin II Peptide Analogues: A Proposed Key Role of the N-Terminal Region for Novel Urotensin II Receptor Modulators. J Med Chem. 2024 Aug 22;67 (16) :13879-13890.