Ulimorelin

Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition[1][2][3].

Product Specifications

CAS Number

[842131-33-3]

Product Name Alternative

TZP-101

UNSPSC

12352005

Target

Adrenergic Receptor; GHSR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/ulimorelin.html

Purity

96.10

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(N(C)[C@H](C)C(N[C@@H]1CC2=CC=C(F)C=C2)=O)[C@H](C3CC3)NC[C@@H](C)OC4=CC=CC=C4CCCNC1=O

Molecular Formula

C30H39FN4O4

Molecular Weight

538.65

References & Citations

[1]Pustovit RV, et al. The mechanism of enhanced defecation caused by the ghrelin receptor agonist, ulimorelin. Neurogastroenterol Motil. 2014 Feb;26 (2) :264-71.|[2]Broad J, et al. Analysis of the ghrelin receptor-independent vascular actions of ulimorelin. Eur J Pharmacol. 2015 Apr 5;752:34-9. |[3]Hoveyda HR, et al. Optimization of the potency and pharmacokinetic properties of a macrocyclic ghrelin receptor agonist (Part I) : Development of ulimorelin (TZP-101) from hit to clinic. J Med Chem. 2011 Dec 22;54 (24) :8305-20.