| Bioactivity | 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]. |
| 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: |
| Name | Ulimorelin |
| CAS | 842131-33-3 |
| Formula | C30H39FN4O4 |
| Molar Mass | 538.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
Ulimorelin
CAS: 842131-33-3 F: C30H39FN4O4 W: 538.65
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a proki
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