UlimorelinUlimorelin
MedChemExpress (MCE)
HY-14903
842131-33-3
TZP-101
96.10%
Powder -20掳C 3 years In solvent -80掳C 6 months -20掳C 1 month
Room temperature in continental US
may vary elsewhere.
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 伪1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.
Ulimorelin (TZP-101
0.3-5 mg/kg
i.v.) causes a dose dependent increase in the numbers and amplitudes of phasic pressure waves recorded from the colorectum[1]. Ulimorelin (1, 3, 5 mg/kg
i.v.) causes a substantial and prolonged (~1 h) increase in colorectal propulsive activity and expulsion of colonic contents[1]. Ulimorelin (p.o.
8 mg/kg) has a Cmax of 0.39 渭M and a AUC of 82 渭M鈥in for rats. Ulimorelin (i.v.
2 mg/kg) has a T1/2 of 50 mins, a CL of 24 mL/min/kg, and a Vss of 1.7 L/kg for rats[3].
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[1]. Pustovit RV, et al. The聽mechanism聽of聽enhanced聽defecation聽caused聽by the聽ghrelin聽receptor聽agonist,聽ulimorelin. Neurogastroenterol Motil.聽2014 Feb
26(2):264-71. [Content Brief]
[2]. Broad J, et al. Analysis of the ghrelin receptor-independent vascular actions of ulimorelin. Eur J Pharmacol.聽2015聽Apr 5
752:34-9.聽 [Content Brief]
[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. [Content Brief]