Ulimorelin

Modify Date: 2024-01-09 16:05:16

Ulimorelin Structure
Ulimorelin structure
Common Name Ulimorelin
CAS Number 842131-33-3 Molecular Weight 538.65300
Density N/A Boiling Point N/A
Molecular Formula C30H39FN4O4 Melting Point N/A
MSDS N/A Flash Point N/A
Purity Quantity Budget Inquiry

 Use of 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].

 Names

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

 Ulimorelin Biological Activity

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
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.

 Chemical & Physical Properties

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

 Synonyms

Ulimorelin
TZP 101
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