Ulimorelin  (Synonyms: TZP-101)

Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC₅₀ of 29 nM and a K_i 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].

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 C_max of 0.39 μM and a AUC of 82 μM•min for rats. Ulimorelin (i.v.; 2 mg/kg) has a T_1/2 of 50 mins, a CL of 24 mL/min/kg, and a V_ss of 1.7 L/kg for rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

538.65

C₃₀H₃₉FN₄O₄

842131-33-3

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

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• [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.  [Content Brief]

  [2]. Broad J, et al. Analysis of the ghrelin receptor-independent vascular actions of ulimorelin. Eur J Pharmacol. 2015 Apr 5;752:34-9.   [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]