842131-33-3

842131-33-3 structure

Name: Ulimorelin
Chemical Name: D-Phenylalanine, (2S)-N-[(2R)-2-[2-(3-aminopropyl)phenoxy]propyl]-2-cyclopropylglycyl-N-methyl-D-alanyl-4-fluoro-, (3→1)-lactam
CAS Number: 842131-33-3
Molecular Formula: C₃₀H₃₉FN₄O₄
Molecular Weight: 538.65300
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2016-03-03 02:53:38
Modify Date: 2025-08-25 17:14:06
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].

Name	D-Phenylalanine, (2S)-N-[(2R)-2-[2-(3-aminopropyl)phenoxy]propyl]-2-cyclopropylglycyl-N-methyl-D-alanyl-4-fluoro-, (3→1)-lactam
Synonyms	Ulimorelin TZP 101

Description	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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Metabolic Disease Signaling Pathways >> GPCR/G Protein >> GHSR
In Vivo	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 μM and a AUC of 82 μM•min 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]. Animal Model: Male Sprague-Dawley rats[1] Dosage: 0.3, 1, 3, 5 mg/kg Administration: i.v. Result: Caused a dose dependent increase in the numbers and amplitudes of phasic pressure waves recorded from the colorectum.
References	[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.

Molecular Formula	C₃₀H₃₉FN₄O₄
Molecular Weight	538.65300
Exact Mass	538.29600
PSA	99.77000
LogP	3.52230

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